All New Products Listed Chronologically

Cat.No. Product Name Information Added
S8905 MYCi361 MYCi361 is a MYC inhibitor that engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 binds to MYC with Kd of 3.2 μM. MYCi361 suppresses in vivo tumor growth, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy. Jul 08 2020
S8845 GSK3145095 GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities. Jul 08 2020
S2654 Neoruscogenin Neoruscogenin, a natural sapogenin isolated from R. rhizoma, is a potent and high-affinity agonist of RAR-related orphan receptor alpha (RORα or nuclear receptor NR1F1). Jul 08 2020
S0718 AG-120 (racemic) AG-120 (racemic), the racemic mixture of AG-120, is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity. Jul 06 2020
S0018 Verdiperstat Verdiperstat (AZD3241) is a selective, orally active and irreversible inhibitor of myeloperoxidase (MPO) with IC50 of 630 nM. Verdiperstat (AZD3241) can be used in the research of neurodegenerative brain disorders. Jul 06 2020
S0277 BMS303141 BMS-303141 is a potent, cell-permeable inhibitor of ATP-citrate lyase (ACL) with IC50 of 0.13 μM. BMS-303141 shows inhibition of total lipid syntheses with IC50 of 8 μM in HepG2 cells. Jul 06 2020
S7321 FIPI FIPI, a derivative of halopemide, is a potent and selective inhibitor of phospholipase D with IC50 of 25 nM and 20 nM for PLD1 and PLD2, respectively. Jul 06 2020
S0308 AMZ30 AMZ30 is a selective and covalent inhibitor of protein phosphatase methylesterase-1(PME-1) with IC50 of 0.60 μM. AMZ30 reduces the demethylated form of PP2A in living cells. Jul 06 2020
S0555 Adomeglivant Adomeglivant is a potent and selective antagonist of glucagon receptor that is used as a chronic treatment for type 2 diabetes. Jul 06 2020
S0078 1V209 (TLR7 agonist T7) 1V209 (TLR7 agonist T7) is an agonist of Toll-like receptor 7 (TLR7) with anti-tumor effects. 1V209 can be used as vaccine adjuvants, enhances antigen specific humoral and cellular immune responses. Jul 06 2020
S2176 Tenovin-3 Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells. Jul 06 2020
S0088 Pemigatinib (INCB054828) Pemigatinib (INCB054828) is an orally active and selective inhibitor of FGFR with IC50 of 0.4 nM, 0.5 nM, 1.2 nM and 30 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma. Jul 06 2020
S6597 TLR2-IN-C29 TLR2-IN-C29 (C29) is a Toll-like receptor 2 (TLR2) inhibitor that inhibits TLR2/1 and TLR2/6 signaling. Jul 06 2020
S0338 NB 598 NB-598 is a potent, competitive squalene epoxidase (SE) inhibitor. NB-598 suppresses cholesterol biosynthesis. Jul 06 2020
S6845 GRL0617 GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLPro)/deubiquitinase with IC50 of 0.6 μM and Ki of 0.49 μM. GRL0617 inhibits SARS-CoV viral replication in Vero E6 cells with EC50 of 15 microM and has no associated cytotoxicity. Jul 06 2020
S0177 XMD-17-51 XMD-17-51 is a potent and highly selective inhibitor of NUAK1. Jul 06 2020
S8730 BAY 1251152 BAY1251152 is a potent PTEFb/CDK9 inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins. Jul 06 2020
S0178 GLX351322 GLX351322 is a NADPH oxidase 4 (NOX4) inhibitor. GLX351322 inhibits hydrogen peroxide production from tetracycline inducible NOX4-overexpressing cells with IC50 of 5 μM. Jul 06 2020
S0425 TBK1/IKKε-IN-2 TBK1/IKKε-IN-2 is a dual inhibitor of TBK1 and IKKε. Jul 06 2020
S0201 Z-JIB-04 (NSC 693627) Z-JIB-04 (NSC 693627) is an isomer of JIB-04. JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 of 230 nM, 340 nM, 855 nM, 445 nM, 435 nM, 1100 nM and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively. Jul 06 2020
Cat.No. Product Name Information Added
S0485 Hoechst 33342 Hoechst 33342 is a membrane-permeant fluorescent stain that can stain live cells. Hoechst 33342 binds to adenine-thymine-rich regions of DNA in the minor groove. Jul 06 2020
S7794 JNK Inhibitor VIII JNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively. Jul 01 2020
S8885 UT-34 UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) pan antagonist and degrader with IC50 of 203.46 nM, 80.78 nM and 94.17 nM for wild-type, T877A and W741L AR, respectively. UT-34 is a potential next-generation therapeutic for enzalutamide-resistant prostate cancer. Jul 01 2020
S8953 ASP4132 ASP4132 is a potent and orally active activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK) with EC50 of 0.018 μM. ASP4132 is used as a clinical candidate for the treatment of human cancer. Jul 01 2020
S8900 SR18662 SR18662 is an optimized compund based on ML264 that inhibits Krüppel-like factor 5 (KLF5) with IC50 of 4.4 nM. SR18662 reduces the viability of multiple colorectal cancer cell lines. SR18662 induces apoptosis. Jul 01 2020
S8945 BAY-1816032 BAY-1816032 is a potent and oral available inhibitor of budding uninhibited by benzimidazoles 1 (BUB1) kinase with IC50 of 6.1 nM for recombinant catalytic domain of human BUB1. BAY-1816032 has antitumor activity. Jul 01 2020
S8889 MZ-1 MZ-1 is a PROTAC degrader of bromodomain-containing protein 4 (BRD4). MZ-1 binds to the Brd bromodomain with Kd of 62 nM, 60 nM, 21 nM, 13 nM, 39 nM and 15 nM for Brd2BD1, Brd2BD2, Brd3BD1, Brd3BD2, Brd4BD1 and Brd4BD2. Jul 01 2020
S6849 DFO DFO (1,8-diazafluoren-9-one) is a fluorochrome that is used in the forensic field to enhance latent fingerprints deposited on porous surfaces by reacting with the amino acids present in the papillary exudate. Jul 01 2020
S9608 AB928 AB928 is a novel dual A2aR/A2bR antagonist with Kd of 1.4 nM and 2 nM for A2aR and A2bR, respectively. Jun 30 2020
S0769 MMP-9-IN-1 MMP-9-IN-1 is a specific inhibitor of matrix metalloproteinase-9 (MMP-9). MMP-9-IN-1 selectively targets the hemopexin (PEX) domain of MMP-9 with Kd of 2.1 μM. Jun 29 2020
S0788 ML 210 ML-210 is a selective covalent inhibitor of cellular glutathione peroxidase 4 (GPX4) with EC50 of 0.04 μM and induces ferroptosis. ML-210 can selectively kill cells induced to express mutant RAS. ML-210 exhibits anti-cancer activity. Jun 29 2020
S0136 KY-226 KY-226 is a potent, selective, orally active and allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 μM for human PTP1B activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. Jun 29 2020
S8815 BSJ-03-123 BSJ-03-123 is a phthalimide-based degrader of cyclin-dependent kinase 6 (CDK6). (PROTAC) Jun 29 2020
S8017 WIN 55, 212-2 mesylate WIN 55,212-2 Mesylate is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission. Jun 29 2020
S8980 SBI-797812 SBI-797812 is a NAMPT activator which is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT. SBI-797812 turns NAMPT into a "super catalyst" that more efficiently generates NMN. Jun 24 2020
S8995 BAY 2416964 BAY 2416964 (compound 192) is a potent and orally active antagonist of aryl hydrocarbon receptor (AhR) with IC50 of 341 nM. BAY 2416964 has the potential in the treatment of solid tumors. Jun 24 2020
S0118 SBC-110736 SBC-110736 is an inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9) that lowers cholesterol levels in mice. Jun 23 2020
S6848 3'-Fluoro-3'-deoxythymidine (Alovudine) 3'-Fluoro-3'-deoxythymidine (Alovudine) is a potent inhibitor of polymerase γ and reverse transcriptase that can be used in the treatment of HIV infection. 3'-Fluoro-3'-deoxythymidine (Alovudine) is also a marker of DNA synthesis that can be used as an early response biomarker in the chemotherapy of pancreatic cancer. Jun 22 2020
S6559 ML-297 ML-297 is a potent and selective activator of Kir3.1/3.2 (G protein-coupled inwardly rectifying potassium, GIRK1/2) channel with EC50 of 0.16 μM and 1.8 μM for GIRK1/2 and GIRK1/4, respectively. ML-297 is potential for the treatment of epilepsy. Jun 15 2020
S6615 ATB 346 ATB 346, a novel hydrogen sulphide-releasing derivative of naproxen with remarkably reduced toxicity, inhibits COX activity. ATB 346 is an anti-inflammatory agent that induces apoptosis of human melanoma cells. Jun 15 2020
Cat.No. Product Name Information Added
S0102 L 189 L 189 is a novel human DNA ligase inhibitor with IC50 of 5 μM, 9 μM and 5 μM for hLigI, hLigIII and hLigIV, respectively. L 189 inhibits base excision repair (BER) and non-homologous end joining (NHEJ). L 189 specifically sensitizes cancer cells to DNA damage. Jun 15 2020
S0129 SB-297006 SB-297006 is an antagonist of C-C chemokine receptor 3 (CCR3) that suppresses antigen-induced accumulation of T(h)2 as well as eosinophils in the lungs. SB-297006 suppressed CCL11-induced Th2 chemotaxis with IC50 of 2.5 μM. Jun 15 2020
S0103 ML327 ML327 is an isoxazole compound that blocks MYC expression and tumor formation in neuroblastoma. ML327 also restores E-cadherin expression with In-Cell Western EC50 of 1.0 μM. ML327 induces apoptosis. Jun 08 2020
S4307 Auranofin Auranofin (SKF-39162) is an inhibitor of thioredoxin reductase (TrxR) with IC50 of 88 nM for purified H. pylori TrxR in cell-free assay. Auranofin has anti-cancer activity and can completely inhibit bacterial growth at 1.2 μM. Auranofin is an FDA-approved gold-containing compound used for the treatment of rheumatoid arthritis. Jun 08 2020
S0154 CAY10465 CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM. Jun 08 2020
S6771 MAC-545496 MAC-545496 is a nanomolar glycopeptide-resistance-associated protein R(GraR) inhibitor with strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 can reverse β-lactam resistance in methicillin-resistant strains and synergize with CAMPs. MAC-545496 shows remarkable activity in macrophages and attenuates S. aureus virulence in a G. mellonella larvae infection model. Jun 08 2020
S8852 Pyrotinib (SHR-1258) Pyrotinib (SHR-1258) is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively. Jun 08 2020
S0443 Desciclovir Desciclovir (DCV) is a prodrug of the antiherpetic agent acyclovir (ACV) that converted into ACV by xanthine oxidase in humans. Jun 08 2020
S7688 Ki20227 Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively. Jun 03 2020
S8961 Alobresib (GS-5829) Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling. Jun 03 2020
S6805 Tyrphostin AG-528 Tyrphostin AG-528 is a potent inhibitor of epidermal growth factor receptors (EGFR) and ErbB2/HER2 with IC50 of 4.9 μM and 2.1 μM, respectively. Tyrphostin AG-528 exhibits anticancer activity. Jun 03 2020
S6844 BPN14770 BPN14770 is a selective allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively. Jun 03 2020
S7692 A-83-01 A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions are best fresh-prepared. Jun 03 2020
S6832 MC-VC-PAB-PNP MC-Val-Cit-PAB-PNP is a cathepsin cleavable ADC peptide linker that is applicable to the synthesis of antibody-drug conjugates (ADCs). Jun 03 2020
S6841 RU.521 RU.521 is an active, potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS) that inhibits the cGAS-mediated signaling with IC50 of 700 nM. RU.521 binds to the cGAS/dsDNA complex with Kd of 36.2 nM. Jun 03 2020
S6838 BCTC BCTC is an orally effective and highly potent vanilloid receptor 1 (VR1/TRPV1) antagonist. BCTC inhibits capsaicin-induced and acid-induced activation of rat VR1 with IC50 of 35 nM and 6.0 nM, respectivley. BCTC exhibits anti-tumor activity. Jun 03 2020
S6843 X-82 (Vorolanib) Vorolanib is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities. Jun 03 2020
S8883 LLY-283 LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity. Jun 03 2020
S6842 MF-438 MF-438 is a potent and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor with IC50 of 2.3 nM for rSCD1. Jun 03 2020
S8951 TED-347 TED-347 is a potent, irreversible, covalent and allosteric inhibitor of the TEAD⋅Yap protein-protein interaction. TED-347 inhibits TEAD4⋅Yap1 protein-protein interaction with an apparent EC50 of 5.9 μM. Jun 03 2020
Cat.No. Product Name Information Added
S6840 OSU-T315 OSU-T315 is a potent Integrin-Linked Kinase (ILK) inhibitor with IC50 of 0.6 μM. OSU-T315 induces autophagy and apoptosis, both of which are integral to its antiproliferative activity. OSU-T315 exhibits anti-tumor activity. Jun 03 2020
S0276 GSK-2881078 GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia. Jun 02 2020
S0523 SB 4 (Eticovo) SB 4 (Eticovo) is a potent and selective agonist of bone morphogenetic protein 4 (BMP4) signaling with EC50 of 74 nM. SB 4 (Eticovo) enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation. Jun 02 2020
S0039 BI-409306 BI 409306 is a potent and selective inhibitor of human and rat PDE9A with mean IC50 of 65 nM and 168 nM, respectively. Treatment with BI 409306 increases brain cGMP levels, promotes long-term potentiation, and improves episodic and working memory performance in rodents. Jun 02 2020
S0295 Anavex 2-73 HCl Anavex 2-73, an aminotetrahydrofuran derivative, is a mixed muscarinic and sigma-1/σ1 Receptor agonist with IC50 of 0.86 μM. Jun 02 2020
S0302 F1063-0967 F1063-0967 is an inhibitor of Dual-specificity phosphatase 26 (DUSP26) with IC50 of 11.62 μM. Jun 02 2020
S0313 Volinanserin Volinanserin is a highly selective and potent 5-HT2 receptor antagonist with Ki of 0.36 nM. Volinanserin shows antipsychotic activity. Jun 02 2020
S0779 Pirenperone Pirenperone, a quinazoline derivative, is a selective antagonist of SR-2A (5-HT2 serotonin receptor) when employed in low doses. Pirenperone behaves like a typical neuroleptic when used in higher doses (greater than 0.1 mg/kg). Jun 02 2020
S0096 S-Gboxin S-Gboxin, a functional analogue of Gboxin, is an oxidative phosphorylation (OXPHOS) inhibitor which inhibits growth of mouse and human glioblastoma (GBM) with IC50 of 470 nM. Jun 02 2020
S8879 BMS-986165 BMS-986165 is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases. Jun 02 2020
S8858 GSK3368715 (EPZ019997) 3HCl GSK3368715 is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM. Jun 02 2020
S0209 BVT 2733 BVT 2733, a new small molecule, is a non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1). Jun 02 2020
S0487 Sulfatinib Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs. Jun 02 2020
S0500 Purvalanol B Purvalanol B (NG-95) is a potent and selective inhibitor of cyclin-dependent kinase (CDK) with IC50 of 6 nM, 6 nM, 9 nM and 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. May 26 2020
S0528 Raphin1 Raphin1 is an orally bioavailable, selective inhibitor of R15B (PPP1R15B, a regulatory subunit of protein phosphatase 1). Raphin1 binds strongly to the R15B-PP1c holophosphatase with Kd of 33 nM. May 26 2020
S0287 P7C3-A20 P7C3-A20 is a highly active analogue of P7C3. P7C3-A20 is neuroprotective and promotes endogenous reparative strategies after TBI (Traumatic brain injury). May 26 2020
S0328 MMAF MMAF (Monomethylauristatin F) is a synthetic antineoplastic agent and a potent inhibitor of tubulin polymerization. MMAF (Monomethylauristatin F) is applied as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin, ABT-414 and SGN-CD19A. May 26 2020
S7969 THZ2 THZ2, a THZ1 analog, is a selective inhibitor of CDK7 with IC50 of 13.9 nM. THZ2 efficiently suppresses the clonogenic growth of TNBC cells with IC50 of ~10 nM. May 26 2020
S6836 TH-257 TH-257 is a potent and exquisitely selective LIM kinase (LIMK) inhibitor with IC50 of 84 nM and 39 nM for LIMK1 and LIMK2, respectively. May 26 2020
S8943 VLX600 VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity. May 26 2020
Cat.No. Product Name Information Added
S8947 SX-682 SX-682 is an orally bioavailable small-molecule allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor MDSC recruitment and enhances T cell activation and antitumor immunity. May 26 2020
S8903 AS2863619 AS2863619 is a small-molecule cyclin-dependent kinase CDK8/19 inhibitor with IC50 of 0.6099 nM and 4.277 nM, respectively. AS2863619 is a potent Foxp3 inducer in Tconv cells. May 26 2020
S6806 SBI-115 SBI-115 is a novel TGR5 (GPCR19) antagonist. SBI-115 decreases cell proliferation, cholangiocyte spheroid growth and cAMP levels in cystic cholangiocytes. May 26 2020
S0391 TG-89 TG-89 is a JAK inhibitor that inhibits JAK2, FLT3, RET and JAK3. May 26 2020
S0435 PF-9366  PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor with IC50 of 420 nM and Kd of 170 nM. May 26 2020
S0436 Pleconaril Pleconaril is a capsid inhibitor used previously to treat enterovirus infections. Pleconaril is effective in inhibiting replication with IC50 of < 0.050 μM. May 26 2020
S0469 ML216 ML216 is a potent and selective inhibitor of the DNA unwinding activity of BLM(Bloom’s syndrome protein) with antitumor activity. ML216 inhibits helicases with IC50 of 0.97 μM and 2.98 μM for BLM636-1298 and BLMfull-length, respectively. May 26 2020
S0470 RSV604 RSV604, a novel benzodiazepine, is an inhibitor of respiratory syncytial virus (RSV) with EC50 of 0.86 μM. RSV604 has significant potential for the effective treatment of RSV disease. Phase 2. May 26 2020
S0230 NVP-VID-400 NVP-VID-400 (SDZ285428) is an inhibitor of CYP51. NVP-VID-400 (SDZ285428) inhibits T. cruzi and T. brucei with I/E2a(5 min) of both <1 and I/E2(60 min) of 9 and 35, respectively. May 26 2020
S4922 NSC 632839 NSC 632839 is not only a DUB inhibitor, but also a deSUMOylase inhibitor, it inhibits USP2, USP7, and SENP2 with IC50 of 45 μM, 37 μM, and 9.8 μM, respectively. May 25 2020
S4327 Famprofazone Famprofazone is a non-steroidal anti-inflammatory agent (NSAID) of the pyrazolone series. Famprofazone is an analgesic used for fever and pain relief. Famprofazone can be metabolized to methamphetamine and amphetamine following administration. May 25 2020
S4339 Meticrane Meticrane is a diuretic that inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. Meticrane is used to treat essential hypertension. May 25 2020
S8851 Elexacaftor (VX-445) Elexacaftor (VX-445) is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector.This is a compound which is not chiral purity. May 25 2020
S4389 Bephenium Hydroxynaphthoate Bephenium is an activator of B-type Acetylcholine receptor (AChR). Bephenium selectively activates the Hco-L-AChR1 subtype made of Hco-UNC-29.1, Hco-UNC-38, Hco-UNC-63, Hco-ACR-8 subunits. Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis. May 25 2020
S4397 Diperodon HCl Diperodon, a local anaesthetics, is decomposed by the action of hydrolazes in blood serum. May 25 2020
S4402 Oxeladin Citrate Oxeladin citrate, a cough suppressant, is a highly potent and effective drug applied in the treatment of all types of cough of various etiologies. May 25 2020
S4408 Procodazole Procodazole is used as a potentiator which is non-specific active immunoprotective against viral and bacterial infections. May 25 2020
S8963 HLM006474 HLM006474 is a small molecule pan-E2F inhibitor that inhibits DNA binding to E2F4 with IC50 of 29.8 µM in A375 cells. HLM006474 induces a reduction in cell proliferation and an increase in apoptosis. The CDK/Rb/E2F pathway is commonly disrupted in lung cancer, and HLM006474 is shown to have efficacy in lung cancer. May 20 2020
S6837 R-10015 R-10015 is a potent, selective inhibitor of LIM domain kinase (LIMK) with IC50 of 38 nM for human LIMK1. R-10015 binds to the ATP-binding pocket and acts as a broad-spectrum antiviral compound for HIV infection. May 20 2020
S8969 EIDD-2801 EIDD-2801 is an orally bioavailable prodrug of the ribonucleoside analog β-d-N4-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19. May 20 2020
Cat.No. Product Name Information Added
S0269 GSK467 GSK467 is a cell penetrant and selective inhibitor of KDM5B (JARID1B/PLU1) with Ki of 10 nM. GSK467 shows apparent 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other JmJ family members. May 19 2020
S0285 Bay 41-4109 racemate BAY 41-4109 racemate is a mixture of R-isomer of BAY 41-4109 and S-isomer of BAY 41-4109. BAY 41-4109 an antiviral compound that inhibits human hepatitis B virus (HBV) with IC50 of 53 nM. May 19 2020
S0038 AB-423 AB-423, a member of the sulfamoylbenzamide (SBA) class of hepatitis B virus (HBV) capsid inhibitors, shows potent inhibition of HBV replication with EC50 of 0.08 μM - 0.27 μM and EC90 of 0.33 μM - 1.32 μM in cells. Phase 1. May 19 2020
S0108 AZ-33 AZ-33 is a potent inhibitor of lactate dehydrogenase A (LDHA) with IC50 of 0.5 μM. LDHA is the key enzyme involved in anaerobic glycolysis which is frequently deregulated in human malignancies. May 19 2020
S0360 EGFR Inhibitor EGFR inhibitor, a cell permeable, 4,6-disubstituted pyrimidine compound, is a highly selevtive inhibitor of EGFR kinase with IC50 of 21 nM. EGFR inhibitor directly depolymerizes microtubules and is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics. May 19 2020
S0119 PTP1B-IN-2 PTP1B-IN-2 (MDK3465) is a potent and selective protein tyrosine phosphatase-1B (PTP1B) inhibitor with IC50 of 50 nM. PTP1B-IN-2 enhances insulin-mediated insulin receptor β (IRβ) phosphorylation and insulin-stimulated glucose uptake. May 19 2020
S0160 Toloxatone (MD69276) Toloxatone (MD 69276) is a reversible inhibitor of monoamine oxidase A (MAO-A) with IC50 of  0.93 µM. Toloxatone is an antidepressant agent. May 19 2020
S0184 XY1 XY1 is an inactive, close analog of SGC707 that can be used as the negative control for SGC707. SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively. May 19 2020
S8876 RK-287107 RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM. May 19 2020
S0462 NS-1619 NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels. May 19 2020
S0222 Lvguidingan Lvguidingan (Anticonvulsant 7903) is an anticonvulsant/antiepileptic agent. Lvguidingan (Anticonvulsant 7903) is found to be able to increase the concentration of 5-HT and 5-HIAA in mice brain. May 19 2020
S0471 TD-139 TD-139 is a potent and selective inhibitor of galectin-3 with Kd of 0.036 µM over galectin-1 and galectin-7 with Kd of 2.2 µM and 32 µM, respectively. TD-139 is used potentially for the treatment of idiopathic pulmonary fibrosis (IPF). May 19 2020
S8892 JHU395 JHU395 is a novel orally bioavailable GA (glutamine antagonists) prodrug designed to circulate inert in plasma, but permeate and release active GA within target tissues. JHU395 delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and significantly inhibits tumor growth without observed toxicity. May 14 2020
S8962 BRD3308 BRD3308 is a potant and highly selective inhibitor of HDAC3 with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release. May 14 2020
S8922 TBK1/IKKε-IN-1(compound 1) TBK1/IKKε-IN-1 (compound 1) is a dual inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase-ε (IKKε/IKK-i) with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo. May 14 2020
S7770 1-Methoxy PMS 1-methoxy PMS is stable electron-transport mediator between NAD(P)H and tetrazolium dyes. May 09 2020
S8933 ONO-7475 ONO-7475 is a potent, selective, and orally active novel inhibitor of Anexelekto(Axl)/MER tyrosine kinase with IC50 of 0.7 nM and 1.0 nM for AXL and MER, respectively. ONO-7475 suppresses the emergence and maintenance of tolerant cells to the initial EGFR-TKIs, osimertinib or dacomitinib, in AXL-overexpressing EGFR-mutated NSCLC cells. ONO-7475 arrests growth and kills FMS-like tyrosine kinase 3-internal tandem duplication mutant acute myeloid leukemia cells. May 07 2020
S8532 ARV-771 ARV-771 is a potent pan-(bromodomain and extra-terminal)BET degrader, a novel BET-PROTAC(proteolysis-targeting chimera) with Kd of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively. May 07 2020
S2435 Sodium stibogluconate Sodium stibogluconate, a pentavalent antimony derivative, is a potent and selective inhibitor of protein tyrosine phosphatase (PTPase). Sodium stibogluconate inhibits 99% of Src homology 2 domain-containing phosphatase 1 (SHP-1) activity at 10 μg/ml and similar degrees of inhibition of SHP-2 and PTP1B requires 100 μg/ml. Sodium stibogluconate is a drug used in treatment of leishmaniasis. May 07 2020
S1050 TCS PIM-1 1 TCS PIM-1 1 is a potent and selective inhibitor of ATP-competitive Pim-1 kianse with IC50 of 50 nM, shows good selectivity over Pim-2 and MEK1/MEK2 with IC50 > 20000 nM. May 07 2020
Cat.No. Product Name Information Added
S2649 SB 200646 SB 200646 (SB 200646A) is a potent, selective and oral-active antagonist of 5-HT2B/2C over 5-HT2A receptor with 50 fold selectivity. The pKi for rat 5-HT2C receptor, rat 5-HT2B receptor and rat 5-HT2A receptor are 6.9, 7.5 and 5.2, respectively. SB 200646 has electrophysiological and anxiolytic properties in vivo. May 07 2020
S6722 Seclidemstat (SP-2577) Seclidemstat (SP-2577) is a potent and orally bioavailable inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A) with IC50 of 127 nM. Seclidemstat (SP-2577) has potential antineoplastic activity. May 07 2020
S6797 QX77 QX77 is a novel activator of chaperone-mediated autophagy (CMA). QX77 induces the up-regulation of Rab11 expression and up-regulates LAMP2A expression. May 07 2020
S8894 SR-4835 SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 99 nM and Kd of 98 nM for CDK12 and IC50 of 4.9 nM for CDK13. SR-4835 disables triple-negative breast cancer (TNBC) cells. SR-4835 promotes synergy with DNA-damaging chemotherapy and PARP inhibitors. May 07 2020
S6833 BCI-121 BCI-121 is a potent inhibitor of SMYD3 that impairs the proliferation of many kinds of cancer cells. May 07 2020
S7764 WST-8 WST-8 is a water-soluble tetrazolium salt used for assessing cell metabolic activity that produces corresponding formazan dye that absorbs at 460 nm. WST-8 is typically used as a cell viability indicator in cell proliferation assays. Apr 28 2020
S6813 Mobocertinib (TAK788) Mobocertinib (TAK788), an investigational TKI, is a potent, selective preclinical inhibitor of epidermal growth factor receptor (EGFR) and HER2 mutations. Mobocertinib (TAK788) is an antineoplastic agent. Apr 28 2020
S6824 Lucigenin Lucigenin is a fluoerscent probe that exhibits a bluish-green fluorescence in the presence of endogenously generated superoxide anion radicals and chloride in cells. Apr 28 2020
S6825 Thioflavine S Thioflavine S is a fluorogenic compound which becomes fluorescent only after oxidation. Thioflavine S is used as a fluorescent histochemical marker of dense core senile plaques. Apr 28 2020
S6830 o-Phenanthroline o-Phenanthroline, a hypoxia-mimicking agent, is a non-specific matrix metalloproteinase (MMP) inhibitor with IC50 of 110.5μM for Collagenase. O-phenanthroline reduces the expression of MMP3 and MMP13 mRNA levels during chondrogenic differentiation of human chondrocytes (hChs), as well as after TNFα/IL-1β exposure in an explant model. o-Phenanthroline is also a metal chelator which prevents the induction of chromosomal aberrations in streptozotocin-treated cells and forms a red chelate with Fe2+ that absorbs maximally at 510 nm. Apr 28 2020
S6831 HEPES HEPES is a zwitterionic sulfonic acid buffering agent, commonly used to uphold a neutral pH of basal medium within cell cultures. Apr 28 2020
S6819 Luminol Luminol is a versatile chemical exhibiting chemiluminescence with a blue glow, when mixed with an appropriate oxidizing agent. Luminol is uesed in forensic investigations to detect trace amounts of blood at crime scenes and in biological researches to detect copper, iron, and cyanides, as well as specific proteins by western blot. Luminol recently displayes promising applications for the treatment of cancer in deep tissues. Apr 28 2020
S6821 Thiazolyl Blue Thiazolyl Blue (MTT) is a cell-permeable and positively charged colorimetric agent that is widely used to detect reductive metabolism in cells and to measure cell proliferation, cytotoxicity, and apoptosis. Thiazolyl Blue (MTT) is reduced from yellow color to purple formazan in living cells. Apr 28 2020
S6829 Dithiothreitol (DTT) Dithiothreitol (DTT), a small-molecule redox reagent, is a standard agent for reducing disulfide bonds between and within biological molecules. Apr 28 2020
S6818 Nile Red Nile Red is an excellent vital fluorescent stain for the detection of intracellular lipid droplets in the presence of a hydrophobic environment. Nile Red is applied for staining intracellular lipids, hydrophobic domains of proteins and lysosomal phospholipid inclusions. Apr 28 2020
S6826 IPTG IPTG is a galactose and a molecular mimic of allolactose that triggers transcription of the lac operon, stimulating protein expression. Apr 28 2020
S6820 X-GAL X-GAL is a widely used chromogenic β-galactosidase substrate. β-galactosidase cleaves X-gal and produce an insoluble detectable blue compound. X-Gal is applied in blue-white selection of recombinant bacterial colonies with the lac+ genotype. Apr 28 2020
S2431 TMTD (Tetramethylthiuram disulfide) TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide. Apr 28 2020
S6822 TMB dihydrochloride TMB dihydrochloride is an excellent colorimetric substrate for detection of horseradish peroxidase (HRP) labeled probes and is used in staining procedures in immunohistochemistry and in enzyme-linked immunosorbent assays (ELISA). Apr 28 2020
S8898 MLT-748 MLT-748 is a potent, selective and allosteric inhibitor of MALT1 with IC50 of 5 nM, binding at the interface between the caspase and immunoglobulin (Ig3) domains by displacing Trp580 and locking the catalytic site in an inactive state. Apr 28 2020
Cat.No. Product Name Information Added
S8915 C75 C75 is a novel, potent synthetic inhibitor of fatty acid synthase (FAS/FASN) with IC50 of 35 μM and 50 μM in clonogenic assays and spheroid growth assay, respectively. C75 is used as a tool for studying fatty acid synthesis in metabolic disorders and cancer. Apr 28 2020
S6781 Brassinazole Brassinazole is a potent inhibitor of brassinosteroid (BR) biosynthesis with IC50 of ~ 1 μM, that has been developed to probe the myriad functions of brassinosteroids. Brassinosteroids are a class of phytohormones with essential roles in plant growth and development, including the promotion of stem elongation and cell division. Apr 28 2020
S8936 VBIT-12 VBIT-12 is a potent inhibitor of Voltage-dependent anion-selective channel 1 (VDAC1), directly interacting with purified VDAC1, reducing its channel conductance and preventing VDAC1 oligomerization. Apr 22 2020
S8954 STING agonist-1 (G10) STING agonist-1 (G10) is a novel human-specific STING agonist that triggers IFN regulatory factor 3 (IRF3)/ type I interferon (IFN)-associated transcription in human fibroblasts. STING agonist-1 (G10) potently reduces growth of Chikungunya virus (CHIKV) with IC90 of 8.01 μM and blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) with IC90 of 24.57 μM. Apr 22 2020
S6828 Cremophor EL Cremophor EL, a polyethoxylated surfactant, is a formulation vehicle used for various poorly-water soluble drugs, including the anticancer agent paclitaxel (Taxol). Cremophor EL is used in severe anaphylactoid hypersensitivity reactions, hyperlipidaemia, abnormal lipoprotein patterns, aggregation of erythrocytes and peripheral neuropathy. Apr 22 2020
S6827 Methyl-β-cyclodextrin Methyl-β-cyclodextrin is a cholesterol-removing agent mainly used for lipid raft disruption. Methyl-β-cyclodextrin induces caspase-dependent apoptosis in PEL cells and inhibits the growth and invasion of PEL cells without apparent adverse effects, suggesting the potential effective antitumor activities. Apr 22 2020
S6815 CDN1163 CDN1163 is a small molecular allosteric activator of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) that improves Ca2+ homeostasis. Apr 22 2020
S6804 CX546 CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator. Apr 22 2020
S6787 KN-93 KN-93 is a cell-permeable, reversible and competitive inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK-II) with Ki of 2.58 μM at rabbit myocardial CaM kinase activity. Apr 22 2020
S6788 PEO-IAA PEO-IAA is a novel potent auxin antagonist that binds to transport inhibitor response 1/auxin signaling F-box proteins (TIR1/AFBs). PEO-IAA suppresses not only the expression of an auxin-responsive ZmSAUR2 gene, but also gravitropic curvature. Apr 22 2020
S2592 Emapunil (AC 5216) Emapunil(AC-5216) is a novel mitochondrial benzodiazepine receptor/translocator protein (MBR/TSPO) ligand. Emapunil(AC-5216) showes high affinity for MBRs prepared from rat whole brain with Ki of 0.297 nM and IC50 of 3.04 nM and 2.73 nM at rat glioma cells and human glioma cells, respectively. Apr 22 2020
S2595 FK-3311 FK-3311 is a selective, cell-permeable and orally available inhibitor of cyclooxygenase-2 (COX-2) with antiinflammatory. FK-3311 has protective effects against hepatic warm ischemia-reperfusion injury by marked inhibition of TxA2. Apr 22 2020
S8888 GMB-475 GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein. Apr 22 2020
S2646 VU0238429 VU0238429 is the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) with EC50 of 1.16 μM at M5 and both > 30 μM at M1 and M3. VU0238429 shows no potentiator activity at M2 or M4. Apr 22 2020
S6782 Anle138b Anle138b is a novel oligomer modulator and an aggregation inhibitor, blocking the formation of pathological aggregates of prion protein (PrP(Sc)) and of α-synuclein (α-syn) with good oral bioavailability, blood-brain-barrier penetration and no detectable toxicity. Anle138b shows a new approach for disease-modifying therapy in neurodegenerative diseases such as prion and Parkinson's disease. Apr 22 2020
S2650 RN-1734 RN-1734 is a selective transient receptor potential vanilloid 4 (TRPV4) antagonist with IC50 of 2.3 μM, 5.9 μM and 3.2 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. RN-1734 alleviates demyelination and inhibits glial activation and the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells. Apr 15 2020
S6814 GS-441524 GS-441524, a molecular precursor to a pharmacologically active nucleoside triphosphate molecule, is a potent inhibitor of feline infectious peritonitis virus (FIPV) with EC50 of 0.78 μM. Apr 15 2020
S5183 PD 169316 PD 169316 is a potent, selective and cell-permeable p38 MAP kinase inhibitor with IC50 of 89 nM. PD169316 abrogates signaling initiated by both TGFbeta and Activin A. PD169316 shows antiviral activity against Enterovirus71. Apr 15 2020
S6794 Thalidomide-O-COOH (Cereblon ligand 3) Thalidomide-O-COOH (Cereblon ligand 3), a Thalidomide-based Cereblon (CRBN) ligand, is used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs (Proteolysis Targeting Chimera). Apr 15 2020
S2427 Triglycidyl Isocyanurate (Teroxirone) Triglycidyl Isocyanurate, also known as Teroxirone, is a triazene triepoxide with antineoplastic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl Isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. Triglycidyl Isocyanurate is also used in various polyester powder coatings in the metal finishing industry. Apr 15 2020
Cat.No. Product Name Information Added
S6775 TUG-891 TUG-891 is a potent and selective agonist of the long chain free fatty acid (LCFA) receptor 4 (FFA4/GPR120), which demonstrates both potential opportunity and possible challenges to therapeutic agonism. Apr 15 2020
S6776 TM5275 Sodium TM 5275 sodium is an orally bioavailable plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 6.95 μM.. Apr 15 2020
S6778 TM5441 TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 ranging between 9.7 μM and 60.3 μM. TM5441 induces intrinsic apoptosis in several human cancer cell lines. Apr 15 2020
S6779 JBSNF-000088 JBSNF-000088 (6-Methoxynicotinamide), an analog of nicotinamide (NA), is a potent inhibitor of Nicotinamide N-methyltransferase (NNMT) with IC50 of 1.8 µM, 2.8 µM, and 5.0 µM for human NNMT(hNNMT), monkey NNMT (mkNNMT) and mouse NNMT (mNNMT), respectively. Apr 15 2020
S6780 TFAP TFAP is a selective and cell-permeable cyclooxygenase-1 (COX-1) inhibitor with IC50 of 0.8 μM. Apr 15 2020
S6777 NSC95397 NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor with Ki of 32 nM, 96 nM, 40 nM for Cdc25A, Cdc25B and Cdc25C, respectively. NSC 95397 has IC50 of 22.3 nM, 56.9 nM and 125 nM for human Cdc25A, human Cdc25C and Cdc25B, respectively. NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway. Apr 15 2020
S6784 STAT5-IN-1 STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform. Apr 15 2020
S6785 DIM-C-pPhCO2Me DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1)(Nur77) antagonist with antineoplastic activity. Apr 15 2020
S6786 ERK5-IN-2 ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50 of 0.82 μM and 3 μM for ERK5 and ERK5 MEF2D, respectively. Apr 15 2020
S6795 VU0357017 Hydrochloride VU0357017 hydrochloride is a potent, highly selective and CNS-penetrant agonist of M1 which is a subtype of muscarinic acetylcholine receptors (mAChRs). VU0357017 hydrochloride appears to act at an allosteric site to activate the receptor with EC50 of 477 nM and Ki of 9.91 μM. Apr 15 2020
S6796 BTB-1 BTB-1 is a novel, selective and reversible inhibitor of the mitotic motor protein Kif18A with IC50 of 1.69 μM. Apr 15 2020
S6798 ELN484228 ELN484228 is a cell-permeable blocker that targets α-synuclein, a key protein in Parkinson’s disease. Apr 15 2020
S6799 DIM-C-pPhOH DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1)(Nur77) antagonist. DIM-C-pPhOH inhibits tumor growth and mTOR signaling, induces apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively. Apr 15 2020
S6800 Exo1 Exo1 is a reversible inhibitor of exocytosis, induces a rapid collapse of the Golgi to the endoplasmic reticulum and the rapid release of ADP-ribosylation factor (ARF) 1 from Golgi membranes. Apr 15 2020
S6686 SC-560 SC-560 is a highly selective COX-1 inhibitor with IC50 of 9 nM, compared with the IC50 of 6.3 μM for COX-2, nearly 1,000-fold higher than with COX-1. Apr 15 2020
S2477 2'-Deoxy-5-Fluorocytidine 2'-Deoxy-5-fluorocytidine, a pyrimidine analog, is a DNA methyltransferase (DMNT) inhibitor currently in clinical trials for solid tumors. Apr 15 2020
S8670 Vipivotide tetraxetan (PSMA-617) Vipivotide tetraxetan (PSMA-617) is a chemically modified PSMA(prostate-specific membrane antigen) inhibitor with a Ki of 0.37 nM. Apr 09 2020
S2587 Sodium Glucoheptonate Dihydrate Sodium glucoheptonate is used for cleaning metal, mercerizing, paint stripping, and aluminum etching. Apr 08 2020
S2578 1-Phenylbiguanide 1-phenylbiguanide (PBG) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM. Apr 08 2020
S2642 1-Naphthyl PP1(1-NA-PP1) 1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively. Apr 08 2020
Cat.No. Product Name Information Added
S6685 Mavacoxib Mavacoxib is a selective, long-acting cyclooxygenase-2 (COX-2) inhibitor. Mavacoxib is a novel nonsteroidal anti-inflammatory drug (NSAID). Apr 08 2020
S2433 DL-Buthionine-Sulfoximine DL-Buthionine-Sulfoximine is an inhibitor of glutathione (GSH) synthesis. Apr 08 2020
S6807 TA-02 TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2. Apr 08 2020
S6808 SU5205 SU5205 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 9.6 µM. Apr 08 2020
S6809 SU5214 SU5214 is a inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively. Apr 08 2020
S6774 TP-3654 TP-3654 is the second-generation PIM inhibitor with Ki values of 5 nM, 239 nM, and 42 nM for PIM-1, PIM-2 and PIM-3, respectively. Apr 08 2020
S6793 TG4-155 TG4-155 is a potent and selective Prostaglandin Receptor EP2(PTGER2) antagonist with Ki value of 9.9 nM. Apr 08 2020
S2428 Isopropyl myristate Isopropyl myristate is used as a substitute for natural oils in cosmetics and a co-solvent with skin penetration enhancement properties of active ingredients in many topical and transdermal preparations. Isopropyl myristate is a novel pediculicide rinse (50%) and a safe and effective therapy for the treatment of head lice in children and adults. Apr 02 2020
S8944 G150 G150 is a potent and highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with IC50 of 10.2 nM. Apr 02 2020
S2434 IDRA-21 IDRA-21 is a partial allosteric modulator of AMPA receptor desensitization. IDRA-21 is a potent cognition-enhancing drug virtually devoid of neurotoxic liability. Apr 02 2020
S2465 CPI-1189 CPI-1189 is the proapoptotic cytokine tumor necrosis factor (TNF) alpha inhibitor. CPI-1189 intracellularly inhibits the p38 mitogen-activated protein kinase phosphoactivation and shows neuroprotective effects. Apr 02 2020
S2474 Fabomotizole hydrochloride Fabomotizole hydrochloride exhibits anxiolytic and neuroprotective properties. Fabomotizole hydrochloride is a potent sigma1-receptor agonist with IC50 of 7.1 µM and Ki of 5.9 µM. Apr 02 2020
S2488 VTP-27999 TFA VTP-27999 is an orally efficacious, selecitive alkyl amine renin inhibitor with IC50 of 0.47 nM for 0.3 nM of purified recombinant human renin. Apr 02 2020
S2272 Indoprofen Indoprofen is a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor. Indoprofen prevents muscle wasting in aged mice through activation of PDK1/AKT pathway.Indoprofen selectively increases SMN2-luciferase reporter protein and endogenous SMN protein. Apr 02 2020
S2432 Tetramethylthiuram monosulfide Tetramethylthiuram monosulfide is used on a large scale as a catalyst in rubber-processing techniques. Tetramethylthiuram monosulfide possesses a medium-degree toxicity and causes point mutations in strains TA 100 and TA 1535 (Salmonella typhimurium LT 2). Apr 02 2020
S8913 TH5487 TH5487 is a selective active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM. Apr 02 2020
S2418 Frentizole Frentizole is a novel inhibitor of amyloid beta peptide (Abeta) binding alcohol dehydrogenase (ABAD) interaction with IC50 of 200 μM. Frentizole is a nontoxic antiviral and immunosuppressive agent used clinically in rheumatoid arthritis and systemic lupus erythematosus. Apr 02 2020
S2426 Tirapazamine Tirapazamine is a new anticancer drug in solid tumours. Tirapazamine exhibits preferential tumour cell killing and high specific toxicity to cells at low oxygen tensions. Apr 02 2020
S2436 Pranidipine Pranidipine is a new 1,4-dihydropyridine calcium channel blocker. Pranidipine can enhance cyclic GMP-independent nitric oxide-induced relaxation of the rat aorta. Apr 02 2020
S6684 IOX4 IOX4 is a potent and selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with IC50 of 1.6 nM. IOX4 induces HIFα in various mouse tissues and human cell lines. Apr 02 2020
Cat.No. Product Name Information Added
S2213 AMG-47a AMG-47a is a potent, nonselective inhibitor of Lck kinase with IC50 of 3.4 uM and it also inhibits T cell proliferation. AMG-47a exhibit anti-inflammatory activity (ED50) of 11 mg/kg in the anti-CD3-induced production of interleukin-2 (IL-2) in mice. Apr 02 2020
S2600 Fexinidazole Fexinidazole is a 5-nitroimidazole derivative. Fexinidazole is a DNA synthesis inhibitor and the only, all-oral agent for Human African Trypanosomiasis(HAT or sleeping sickness). Apr 02 2020
S2464 Sevoflurane Sevoflurane is a noncompetitive inhibitor of 5-HT3 receptor. Sevoflurane acts as a low-soluble inhalation anesthetics. Apr 02 2020
S2643 4-IPP 4-IPP is an irreversible inhibitor of macrophage migration inhibitory factor (MIF) and a specific suicide substrate for MIF. 4-IPP can inhibit receptor activator of NF-κB ligand (RANKL)-induced osteoclastogenesis and potentiate osteoblast-mediated mineralization and bone nodule formation in vitro. Apr 02 2020
S2441 Estramustine phosphate sodium Estramustine phosphate sodium is an antitumour drug with a unique dual mode of action. Estrone and estradiol, products of the metabolism of estramustine phosphate sodium, have shown antigonadotrophic activity resulting in reduced testosterone levels. Estramustine(the cytotoxic metabolite produced by dephosphorylation of estramustine phosphate sodium) is an antiprostatic tumor drug with antimicrotubule effects. Apr 02 2020
S2307 Roquinimex Roquinimex is a novel immunomodulator augmenting natural killer (NK) cell activity and T-lymphocyte related effector functions. Roquinimex is a potent oral active tumor antiangiogenic agent. Roquinimex inhibits the secretion of TNF-α. Apr 02 2020
S2419 Eprobemide Eprobemide is a reversible monoamine oxidase A (MAO-A) inhibitor. Eprobemide acts as an antidepressant in Russia. Apr 02 2020
S2421 PF-04457845 PF-04457845 is a potent, favorable selective inhibitor of Fatty acid amide hydrolase (FAAH) with IC50 of 7.2 nM and 7.4 nM for hFAAH and rFAAH, respectively. PF-04457845 covalently modifies the active-site serine nucleophile of FAAH with exquisite selectivity relative to other members of the serine hydrolase superfamily. Apr 02 2020
S2444 Parbendazole Parbendazole is an extremely potent inhibitor of microtubule assembly with IC50 of 3 µM for the assembly of brain microtubules. Apr 02 2020
S2644 Lerisetron Lerisetron is a 5-HT3 receptor antagonist with IC50 of 0.81μM. Apr 02 2020
S2645 SIB 1757 SIB 1757 is a highly selective, noncompetitive antagonist of metabotropic glutamate receptor type 5 (mGluR5) with IC50 of 0.4 μM at hmGluR5 compared with >30 µM at hmGluR1b, hmGluR2, hmGluR4, hmGluR6, hmGluR7 and hmGluR8. Apr 02 2020
P1087 Carperitide Acetate (alpha-human atrial natriuretic peptide) Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 1 nM. Mar 25 2020
S8812 CM272 CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, GLP, respectively. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death. Mar 25 2020
S6671 SN50 SN50, a cell-permeable NF-κB inhibitory peptide, is composed of the signal peptide of Kaposi fibroblast growth factor.SN50 inhibits the activation of NF-κB and attenuates ventilator-induced lung injury. Mar 25 2020
S6679 C25-140 C25-140 is a small-molecule inhibitor of TRAF6-Ubc13 interaction. C25-140 directly binds to TRAF6, thereby blocking the interaction of TRAF6 with Ubc13, and as a consequence lowers TRAF6 activity. C25-140 impedes NF-κB activation in various immune and inflammatory signaling pathways also in primary human and murine cells. Mar 25 2020
S8500 BAY1125976 BAY 1125976 is a selective allosteric AKT1/2 inhibitor,exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY1125976 inhibits the activity of AKT1 (IC50 = 5.2 nM at 10 µM ATP and 44 nM at 2 mM ATP) and AKT2 (IC50 = 18 nM at 10 µM ATP and 36 nM at 2 mM ATP) very potently.Whereas BAY1125976 is almost inactive on AKT3 (IC50 = 427 nM at 10 µM ATP). Mar 25 2020
S6689 Merimepodib Merimepodib is a potent, specific, and reversible inosine monophosphate dehydrogenase(IMPDH) inhibitor with antiviral activity against hepatitis C virus (HCV) and a variety of DNA and RNA viruses in vitro.Merimepodib is an immunosuppressive agent. Mar 25 2020
S2255 BMOV BMOV is a potent oral vanadium complex with anti-diabetic properties and insulin-mimicking effects.BMOV is shown to improve cardiac dysfunctions in diabetic models. Mar 25 2020
S6514 SU5408 SU5408 is a potent and selective inhibitor of VEGFR2 Kinase with IC50 of 70 nM. Mar 25 2020
S8927 GSK2983559 (compound 3) GSK2983559 is a potent inhibitor of receptor interacting protein 2 (RIP2) kinase with good kinase specificity. Mar 25 2020
Cat.No. Product Name Information Added
S8926 Valemetostat (DS-3201) Valemetostat is a selective EZH1/2 dual inhibitor. Mar 25 2020
S6687 SIS17 SIS17 is a mammalian histone deacetylase 11 (HDAC 11)-specific inhibitor with IC50 of 0.83 μM. SIS17 inhibits the demyristoylation of HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs. Mar 25 2020
S8955 AMG-510 racemate AMG-510 racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. Mar 18 2020
S6548 NKL 22 NKL 22 is a selective inhibitor of HDAC with IC50 of 78 µM. Mar 17 2020
S1099 SKLB4771 (FLT3-IN-1) SKLB4771 is a potent and selective inhibitor of human receptor-type tyrosine-protein kinase FLT3 with IC50 of 10 nM. Mar 17 2020
S2115 RG 13022 RG-13022 inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM. Mar 17 2020
S6688 Fmoc-Val-Cit-PAB Fmoc-Val-Cit-PAB is a cleavable linker for antibody-drug conjugates (ADC). Mar 17 2020
S1073 BML-210 (CAY10433) BML-210 is a small molecule inhibitor of HDAC.BML-210 inhibits the HDAC4-VP16-driven reporter signal in a dose-dependent manner with an apparent IC50 of ∼5 µM. Mar 17 2020
S6738 TC-H 106 TC-H 106 is a slow, tight-binding inhibitor of class I histone deacetylases(HDAC) with Ki value of 148 nM, about 102 nM, 14 nM for HDAC1, HDAC2, HDAC3, respectively. Mar 17 2020
S6680 L-779450 L-779450 is a highly potent low nanomolar inhibitor of B-raf with IC50 of 10 nM and Kd of 2.4 nM. Mar 17 2020
S2132 SR-4370 SR-4370 is a potent and selective inhibitor of class I HDACs with IC50 of 0.13 µM, 0.58 µM, 0.006 µM, 2.3 µM, 3.7 µM for HDAC 1, HDAC 2, HDAC 3, HDAC 8, HDAC 6, respectively.SR-4370 suppresses AR signaling and in vivo prostate tumor growth. Mar 17 2020
S6769 Curcumin analog C1 Curcumin analog C1 is a potent transcription factor EB (TFEB) activator with promise for the prevention or treatment of Alzheimer's disease. Mar 17 2020
S4163 Doxycycline Hyclate Doxycycline is a member of the tetracycline antibiotics group, and is commonly used to treat a variety of infections. It is also an inhibitor of matrix metallo-proteinases (MMP). Mar 13 2020
S8932 Remdesivir (GS-5734) Remdesivir,a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV. Mar 13 2020
S8392 NCB-0846 NCB-0846 is a novel, orally small-molecule Wnt inhibitor that inhibits TNIK (TRAF2 and NCK-Interacting Kinase) with an IC50 value of 21 nM. Mar 12 2020
S1058 BI-1347 BI-1347 is small molecule inhibitor of Cyclin-dependent kinase 8(CDK8) with IC50 of 1.1 nM. Mar 11 2020
S2039 IRAK inhibitor 6 IRAK inhibitor 6 is a selective Interleukin-1 receptor-associated kinase 4(IRAK4) inhibitor with IC50 of 0.16 μM. Mar 11 2020
S2002 CZC-25146 CZC-25146 is a potent and selective LRRK2 inhibitor with IC50 of 4.76 nM and 6.87 nM for human wild type LRRK2 and G2019S LRRK2, respectively. Mar 11 2020
S2070 ISCK03 ISCK03 is a cell-permeable inhibitor of stem-cell factor (SCF)/c-kit signaling.ISCK03 inhibits SCF-induced c-c-kit phosphorylation and downstream ERK phosphorylation. Mar 11 2020
S2184 WDR5-0103 WDR5-0103 is a small-molecule antagonist of WDR5 (WD40 repeat protein 5) with Kd of 450 nM. Mar 11 2020
Cat.No. Product Name Information Added
S7339 AZD3965 AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM, 6-fold selective over MCT2. Phase 1. Mar 11 2020
S1141 Tanespimycin (17-AAG) Tanespimycin (17-AAG) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 2. Mar 11 2020
S7668 Picropodophyllin (PPP) Picropodophyllin (PPP) is a IGF-1R inhibitor with IC50 of 1 nM. It displays selectivity for IGF-1R and does not coinhibit tyrosine phosphorylation the IR, or of a selected panel of receptors less related to IGF-IR(FGF-R, PDGF-R, OR EGF-R). Picropodophyllin (PPP) induces apoptosis with antineoplastic activity. Mar 11 2020
A2111 Anti-human CD3-InVivo The OKT-3 monoclonal antibody reacts with human CD3ε which is a 20 kDa transmembrane cell-surface protein that belongs to the immunoglobulin superfamily.The OKT-3 antibody has immunosuppressive properties in vivo and has been shown to effectively treat renal, heart and liver allograft rejection. Mar 11 2020
S1054 AG99 AG99 is a potent and selective inhibitor of EGFR. Mar 11 2020
S6681 Paricalcitol Paricalcitol is a selective vitamin D receptor agonist. Paricalcitol suppresses parathyroid hormone mRNA expression and inhibits parathyroid cell proliferation. Pariccitol is used to treat secondary hyperparathyroidism in chronic kidney disease. Mar 11 2020
S6690 TOFA (5-(Tetradecyloxy)-2-furoic acid) TOFA is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA). Inside the cell, TOFA is converted to TOFyl-CoA (5-tetradecyloxy-2-furoyl-CoA), exerting an allosteric inhibition on ACCA. TOFA blocks fatty acid synthesis and induces cell death in a dose-dependent manner. Mar 11 2020
S6682 Bobcat339 Bobcat339 is a selective cytosine-based TET enzyme inhibitor with IC50 of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 can reduce DNA 5-hydroxymethylcytosine abundance by inhibiting TET enzyme function in living cells and provide support for its utility as a viable pharmacological probe. Mar 11 2020
S6683 D-Lin-MC3-DMA (MC3) D-Lin-MC3-DMA is a potent and ionizable cationic lipid. D-Lin-MC3-DMA is used for delivery of siRNA in vivo. Mar 11 2020
S1024 LTI-291 LTI-291 is the first small-molecule activator of Glucocerebrosidase(GCase) for the treatment of parkinson's disease. Mar 11 2020
S6621 CCG215022 CCG215022 serves as a pan-G protein-coupled receptor kinases (GRKs) inhibitor with IC50 of 3.9 μM, 0.15 μM, 0.38 μM for GRK1, GRK2, GRK5, respectively. Mar 11 2020
S6661 VcMMAE VcMMAE,a MMAE derivative with valine-citrulline (Vc) linker,is an antibody-drug conjugate (ADC) with potent antitumor activity. MMAE is a synthetic antineoplastic agent and can be efficiently released from VcMMAE in vitro and exert cytotoxic activity. Mar 11 2020
S4211 Montelukast Sodium Montelukast selectively antagonizes leukotriene D 4 (LTD4) by binding to it so that block the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1.Precipitations may form after reconstitution,solution is best fresh-prepared. Mar 11 2020
S5764 YM 90709 YM 90709 is a novel IL-5 inhibitor which selectively blocks the binding of IL-5 to the IL-5 receptor (IL-5R). Mar 10 2020
A2103 Anti-mouse CTLA-4 (CD152)-InVivo The UC10-4F10-11 monoclonal antibody reacts with mouse CTLA-4 (cytotoxic T lymphocyte antigen-4) also known as CD152. The UC10-4F10-11 antibody has been shown to promote T cell co-stimulation by blocking CTLA-4 binding to the B7 co-receptors, allowing for CD28 binding. Mar 10 2020
A2104 Anti-mouse CD3ε-InVivo The 145-2C11 monoclonal antibody reacts with mouse CD3ε which is a 20 kDa transmembrane cell-surface protein that belongs to the immunoglobulin superfamily. The 145-2C11 antibody has been shown to induce T lymphocyte activation, proliferation, and apoptosis in vitro via binding and stimulating the TCR. When used in vivo the antibody is reported to produce T cell activation, anergy, or death. Mar 10 2020
S7985 PIM447 (LGH447) PIM447 is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>105-fold differential relative to the Ki on PIMs). PIM447 induces apoptosis. Mar 10 2020
S6598 IRAK-1-4 Inhibitor I IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor associated kinase (IRAK) with IC50 values of 0.3 μM and 0.2 μM for IRAK-1 and IRAK-4, respectively. It displays IC50 values >10 µM in a panel of 27 other kinases tested. Mar 09 2020
S6486 ibandronic acid Ibandronic acid is a potent nitrogen-containing bisphosphonate used in both osteoporosis and to prevent the spread of breast cancer to the bones. Mar 09 2020
S1074 Poliumoside Poliumoside exhibits significant inhibition of advanced glycation end product formation with IC50 values of 19.69 µM. In the rat lens aldose reductase assay.Poliumoside exhibits greater inhibitory effects on rat lens aldose reductase(RLAR) with IC50 values of 8.47 µM. Mar 08 2020
Cat.No. Product Name Information Added
S1059 KDM4D-IN-1 KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM. Mar 08 2020
S6678 Yoda1 Yoda1 acts as an agonist for both human and mouse Piezo1(EC50 of 17.1 and 26.6 μM for mouse and human). Yoda1 activates purified Piezo1 channels in the absence of other cellular components. Mar 08 2020
S2211 AG-13958 AG–013958, a VEGFR tyrosine kinase inhibitor, is in clinical development with ST administration for treatment of choroidal neovascularization associated with age–related macular degeneration (AMD). Mar 08 2020
S2212 AIM-100 AIM-100 is a potent small molecule inhibitor of Ack1 with IC50 of 24nM. Mar 08 2020
S2234 BIBF-0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34nM. Mar 08 2020
S2249 PF 4800567 PF 4800567 is a novel and potent inhibitor of casein kinase 1 epsilon (IC50=32 nM) with greater than 20-fold selectivity over casein kinase 1 delta(IC50=711 nM). Mar 08 2020
S1764 Rifampin Rifampin is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections. Mar 08 2020
A2101 Anti-mouse CD4-InVivo Anti-mouse CD4 antibody reacts with mouse CD4, which is a 55 kDa cell surface type I membrane glycoprotein. CD4 is a co-receptor of the T cell receptor (TCR) and assists the latter in communicating with antigen-presenting cells. Mar 06 2020
A2102 Anti-mouse CD8α-InVivo Anti-mouse CD8α reacts with mouse CD8α. CD8 is a transmembrane glycoprotein that acts as a co-receptor for the T cell receptor (TCR). It binds to class I MHC molecules displayed by antigen presenting cells (APC). Mar 06 2020
A2105 Anti-mouse IFNγ-InVivo The R4-6A2 monoclonal antibody reacts with mouse IFNγ (interferon gamma) which is a 20 kDa soluble pleiotropic cytokine and the sole member of the type II class of interferons. The R4-6A2 antibody has been shown to neutralize both natural and recombinant IFNγ. Mar 06 2020
A2114 Anti-mouse NK1.1-InVivo The PK136 monoclonal antibody reacts with mouse NK1.1 also known as CD161b/CD161c, KLRB1, NKR-P1A and Ly-55. Mar 06 2020
A2106 Mouse IgG1 isotype control-InVivo The monoclonal mouse IgG1 K immunoglobulin is ideal for use as a non-reactive isotype-matched control for mouse IgG1 antibodies in most in vivo and in vitro applications. Mar 06 2020
A2107 Anti-mouse CD25 (IL-2Rα)-InVivo The PC-61.5.3 monoclonal antibody reacts with mouse IL-2Rα also known as CD25, Ly-43, p55, or Tac.The PC-61.5.3 antibody has been shown to inhibit the binding of IL-2 to both the low and high affinity IL-2 receptor forms. Additionally, the PC-61.5.3 antibody is commonly used to deplete CD4+FoxP3+ T regulatory cells in vivo. Mar 06 2020
A2108 Anti-mouse CD28-InVivo The PV-1 monoclonal antibody reacts with mouse CD28.The PV-1 antibody has been shown to stimulate the proliferation and cytokine production by activated T and NK cells. Mar 06 2020
A2109 Anti-mouse IL-4-InVivo The 11B11 monoclonal antibody reacts with mouse IL-4 (interleukin-4) which is a multifunctional 14 kDa cytokine.The 11B11 monoclonal antibody has been shown to neutralize the bioactivity of natural or recombinant IL-4. Mar 06 2020
A2110 Anti-mouse CD16/CD32-InVivo The 2.4G2 monoclonal antibody reacts specifically with mouse CD16 (FcγRIII) and CD32 (FcγRII). It has also been reported to react non-specifically via its Fc domain to FcγRI. The 2.4G2 antibody is commonly used in flow cytometry staining experiments to prevent non-specific binding of IgG to the FcγIII and FcγII, and possibly FcγI, receptors prior to staining with antigen specific primary antibodies. Mar 06 2020
A2112 Anti-mouse CD40L (CD154)-InVivo The MR-1 monoclonal antibody reacts with mouse CD154 also known as CD40 ligand. The MR-1 monoclonal antibody has been reported to inhibit in vitro activation of B lymphocytes by blocking the binding of CD154 with CD40 on T helper cells as well as inhibit the formation of germinal centers and disrupt antigen-specific T cell responses. Additionally, the MR-1 antibody blocks interactions of T cells and antigen-presenting cells in vitro and blocks the development of experimental autoimmune disease in vivo. Mar 06 2020
A2113 Anti-human/mouse TGF-β-InVivo The 1D11.16.8 monoclonal antibody reacts with mouse, human, rat, monkey, hamster, canine and bovine TGF-β (transforming growth factor beta) isoforms 1, 2 and 3.The 1D11.16.8 monoclonal antibody is a neutralizing antibody. Mar 06 2020
S8884 MRTX849 MRTX849 is a potent, selective, and covalent KRASG12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling. Mar 05 2020
S6672 PF-05175157 PF-05175157 is a broad-spectrum effective ACC inhibitor with IC50 of 27.0 nM, 33.0 nM, 23.5 nM and 50.4 nM for human ACC1, human ACC2, rat ACC1, and rat ACC2, respectively. Mar 03 2020
Cat.No. Product Name Information Added
S6675 (R)-GNE-140 (R)-GNE-140 is a selective inhibitor of the LDHA and LDHB with IC50s of 3 nM and 5 nM, respectively. The R enantiomer of GNE-140 is 18-fold more potent than S enantiomer. Mar 03 2020
S6673 CCG-222740 CCG-222740 is a Rho/MRTF pathway inhibitor. CCG-222740 decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression. Mar 03 2020
S6676 Ebselen Ebselen is a small-molecule capsid inhibitor of HIV-1 Replication with IC50 of 46.1 nM in TR-FRET assay. Mar 03 2020
S8531 PF-06650833 PF-06650833 is a potent, selective inhibitor of IRAK4 with an IC50 of 0.2 nM. Mar 03 2020
S8881 DS-1001b (DS 1001) DS-1001b is an oral selective inhibitor of mutant IDH1 R132X with potential antineoplastic activity and is designed to penetrate the blood-brain barrier. Mar 03 2020
S8018 Nirogacestat (PF-03084014) Nirogacestat (PF-03084014, PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. Nirogacestat (PF-03084014, PF-3084014) induces apoptosis. Phase 2. Feb 26 2020
S1060 Olaparib (AZD2281) Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations. Feb 26 2020
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2. Feb 26 2020
S8250 79-6 (CID5721353) 79-6 (CID5721353) is a BCL6 inhibitor with Kd value of 138 μM. Feb 26 2020
S8125 Pamapimod Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms. Feb 26 2020
S4921 MNS (3,4-Methylenedioxy-β-nitrostyrene) MNS is a tyrosine kinase inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively. Feb 26 2020
S8724 Lazertinib Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4. Feb 26 2020
S1300 Tegafur (FT-207) Tegafur (FT-207, NSC 148958) is a substance being used in the treatment of some types of cancer. Feb 26 2020
S7028 Duvelisib (IPI-145) Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3. Feb 26 2020
S7302 TEPP-46 (ML265) ML265 is a potent activator of PKM2 in both biochemical (AC50 = 92 nM) and cell-based assays with high selectivity over PKM1, PKR and PKL. Feb 26 2020
S8236 MK-886 MK-886 is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist. Feb 26 2020
S1044 Temsirolimus (CCI-779) Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis. Feb 26 2020
S8759 S55746 S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds. Feb 26 2020
S6349 NADH Disodium Salt Hydrate NADH is a coenzyme that functions as a regenerating electron donor in catabolic processes including glycolysis, β-oxidation and the citric acid cycle. Feb 26 2020
S7650 Peficitinib (ASP015K) Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3. Feb 26 2020
Cat.No. Product Name Information Added
S6659 Rimegepant (BMS-927711) Rimegepant is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist with ki of 0.027 nM. Feb 26 2020
S7795 Iadademstat(ORY-1001)2HCl ORY-1001 (RG-6016) 2HCl is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of <20 nM, with high selectivity against related FAD dependent aminoxidases. Phase 1. Feb 26 2020
S6663 Resmetirom (MGL-3196) Resmetirom is a liver-directed, orally active, selective thyroid hormone receptor β(THR-β) agonist with an EC50 of 0.21 μM,shows 28-fold selective for THR-β over THR-α in a functional assay. Feb 26 2020
S8193 Lanabecestat(AZD3293) Lanabecestat(AZD3293, LY3314814)is an oral beta-secretase 1 cleaving enzyme (BACE) inhibitor with an inhibitory constant Ki of 0.4 nM. Feb 26 2020
S2759 Fimepinostat(CUDC-907) CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1. Feb 26 2020
S1553 Delafloxacin(ABT-492,RX-3341) ABT-492 is a new fluoroquinolone against 155 aerobic and 171 anaerobic pathogens. Feb 26 2020
S8873 Letermovir(AIC246) Letermovir(AIC246, MK-8228) is a novel anti-CMV compound which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors. Feb 26 2020
S8581 Serabelisib (TAK-117) Serabelisib (INK-1117,MLN-1117,TAK-117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase. Feb 26 2020
S2183 Infigratinib (BGJ398) Infigratinib (BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2. Feb 26 2020
S1089 Refametinib (RDEA119) Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively. Feb 26 2020
S8100 K03861 K03861 is a type II CDK2 inhibitor with Kd of 50 nM, 18.6 nM, 15.4 nM, and 9.7 nM for CDK2(WT), CDK2(C118L), CDK2(A144C), and CDK2(C118L/A144C), respectlvely. Feb 26 2020
S2776 Devimistat(CPI-613) CPI-613, a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in NCI-H460 cell line, disrupts tumor cell mitochondrial metabolism. Phase 2. Feb 26 2020
S7252 selinexor(KPT-330) Selinexor (KPT-330) is an orally bioavailable selective CRM1 inhibitor. Phase 2. Feb 26 2020
S2628 Gedatolisib (PKI-587) Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2. Feb 26 2020
S1119 Cabozantinib (BMS-907351) Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway. Feb 26 2020
S6558 Irosustat (BN83495) Irosustat (STX64, BN83495), a tricyclic coumarin sulfamate, is an orally active, nonsteroid-based, irreversible steroid sulfatase inhibitor with an IC50 of 8 nM. Feb 26 2020
S2727 Dacomitinib (PF-00299804) Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay. Dacomitinib inhibits ERBB2 and ERBB4 with IC50 of 45.7 nM and 73.7 nM, respectively. Dacomitinib is effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Dacomitinib inhibits cell growth and induces apoptosis. Phase 2. Feb 26 2020
S7530 Vactosertib Vactosertib  (TEW-7197, EW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1. Feb 26 2020
S7824 Nazartinib (EGF816) Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro. Feb 26 2020
S1151 Ibutamoren mesylate Ibutamoren mesylate (MK-0667, L163191) is a potent, orally active growth hormone (GH) secretagogue. Ibutamoren (Mesylate) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist. Feb 26 2020
Cat.No. Product Name Information Added
S8822 Ligandrol (LGD-4033) Ligandrol (LGD-4033, VK-5211) is a novel nonsteroidal, oral selective androgen receptor modulator with high affinity (Ki of ∼1 nM) and selectivity. Feb 26 2020
S7855 Brilanestrant (GDC-0810) Brilanestrant (GDC-0810, ARN-810) is a potent ER-α binder (ER-α, IC50 = 6.1 nM; ER-β, IC50 = 8.8 nM), a full transcriptional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors. Feb 26 2020
S1470 Orantinib (SU6668) Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3. Feb 26 2020
S1174 Ostarine (GTx-024) MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3. Feb 26 2020
S2841 Bemcentinib(R428) R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective). Feb 26 2020
S8032 PRT062607 (P505-15) HCl PRT062607 (P505-15, BIIB057) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70. Feb 26 2020
S7707 Verdinexor(KPT-335) Verdinexor (KPT-335) is an orally bioavailable, selective XPO1/CRM1 inhibitor. Feb 26 2020
A2005 Pembrolizumab (anti-PD-1) Pembrolizumab (anti-PD-1) is a potent, highly selective, fully humanized immunoglobulin (Ig) G4-kappa monoclonal antibody against PD-1 with potential immune checkpoint inhibitory and antineoplastic activities. MW : 146.286 KD. Feb 26 2020
S8781 Selpercatinib (LOXO-292) Selpercatinib (LOXO-292, ARRY-192) is a potent and specific RET inhibitor with IC50 values of 1 nM, 2 nM, 2 nM, 4 nM, 2 nM, 2 nM for WT RET, RET V804M, RET V804L, RET A883F, RET M918T and RET S891A respectively. Feb 26 2020
P1022 Desmopressin (DDAVP) Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 1 nM. Feb 26 2020
S8753 INCB054329 INCB054329(INCB-054329; INCB-54329) is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively. Feb 26 2020
S2071 Prulifloxacin (NM441) Prulifloxacin, the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent. Feb 26 2020
S7854 Ulixertinib (BVD-523) Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1. Feb 26 2020
S1480 Lomibuvir (VX-222) Lomibuvir (VX-222, VCH-222) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L. Phase 2. Feb 26 2020
S2151 Sonidegib (NVP-LDE225) Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3. Feb 26 2020
S8166 tirabrutinib(ONO-4059) hydrochloride ONO-4059 (GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM. Feb 26 2020
S8853 Belvarafenib Belvarafenib (GDC5573, HM95573, RG6185) is a selective and orally bioavailable pan-RAF kinase inhibitor with IC50 values of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF(V600E) and CRAF kinases, respectively. Feb 26 2020
S2696 Apitolisib (GDC-0980) Apitolisib (GDC-0980, RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Phase 2. Feb 26 2020
S7555 Domatinostat (4SC-202) 4SC-202 is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1. Feb 26 2020
S7007 Binimetinib (MEK162) Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. Phase 3. Feb 26 2020
Cat.No. Product Name Information Added
S8629 Linrodostat(BMS-986205) BMS-986205 is an irreversible inhibitor of IDO1 with an IC50 of 1.7 nM. It inhibits kynurenine production with IC50 values of 1.7, 1.1 and > 2000 in human HeLa, HEK293 expressing human IDO-1 and tryptophan-2, 3-dioxygenase cell-based assays. Feb 26 2020
S7674 Savolitinib(AZD6094) Savolitinib (volitinib, AZD6094, HMPL-504) is a novel, potent, and selective MET inhibitor currently in clinical development in various indications, including PRCC. The IC50 values of this compound for c-Met and p-Met are 5 nM and 3 nM, respectively. It shows exquisite selectivity for c-Met over 274 kinase. Feb 26 2020
S1267 Vemurafenib (PLX4032) Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy. Feb 25 2020
S5753 Setipiprant(ACT-129968) Setipiprant(ACT-129968, KYTH-105) is a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2) that that has been shown to have greater specificity for DP2 (CRTH2) than for DP1. Feb 25 2020
S5306 Forchlorfenuron (CPPU) Forchlorfenuron is a synthetic cytokinin that inhibits septins and exhibits anti-parasitic, anticancer, and anti-angiogenic activities. Feb 25 2020
S7846 Dubermatinib(TP-0903) TP-0903 is a potent and selective AXL Inhibitor with IC50 of 27 nM. Feb 25 2020
S8526 GDC-0575 (ARRY-575) GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM. Feb 25 2020
S2001 Elvitegravir (JTK-303) Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively. Feb 25 2020
S7102 Berzosertib (VE-822) VE-822 is an ATR inhibitor with IC50 of 19 nM in HT29 cells. Feb 25 2020
S7189 Molibresib (I-BET-762) I-BET-762 is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins. Feb 25 2020
S8362 Tucatinib (Irbinitinib, ONT-380) Tucatinib (Irbinitinib, ONT-380) is an oral, potent, selective, reversible and ATP-competitive small-molecule inhibitor of ErbB-2 (also called HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively in cell-based assays, showing ~500-fold selective for HER2 vs EGFR. It has potential antineoplastic activity. Feb 25 2020
S8294 Olmutinib (BI 1482694) Olmutinib is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor (TKI). Also a potent inhibitor of Bruton's tyrosine kinase. Feb 25 2020
S2851 Baricitinib (INCB028050) Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3. Feb 25 2020
S8893 Firsocostat (GS-0976) Firsocostat is a reversible inhibitor of acetyl CoA carboxylase (ACC) with IC50s of 2.1 nM,6.1 nM for hACC1 and hACC2,respectively. Feb 25 2020
S1523 Voxtalisib (XL765) Analogue Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2. Feb 25 2020
S1047 Vorinostat (SAHA) Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification. Feb 25 2020
S6658 ETC-206 (AUM 001) ETC-206 is an orally available highly selective small-molecule MNK 1/2 inhibitor with IC50s of 64 nM and 86 nM, respectively. Feb 25 2020
S1364 Patupilone (Epothilone B) Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2. Feb 25 2020
S1069 Luminespib (NVP-AUY922) Luminespib (AUY-922, NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2. Feb 25 2020
S7766 Cabotegravir (GSK1265744) Cabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2. Feb 25 2020
Cat.No. Product Name Information Added
S1018 Dovitinib (TKI-258) Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4. Feb 25 2020
S7360 Birabresib (OTX015) OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Phase 1. Feb 25 2020
S8540 Voxelotor(GBT440) Voxelotor(GBT440, GTx011) is a novel small molecule hemoglobin modifier which increases hemoglobin oxygen affinity. Feb 25 2020
S8456 VVPS34 inhibitor 1 (Compound 19) VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM. Feb 25 2020
S7646 Voxtalisib (XL765) Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2. Feb 25 2020
S1098 Rucaparib (AG-014699) phosphate Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3. Feb 25 2020
S2772 Dalcetrapib (JTT-705) Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. Phase 3. Feb 25 2020
S2789 Tofacitinib (CP-690550) Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1. Tofacitinib inhibits the expression of antiapoptotic BCL-A1 and BCL-XL in human plasmacytoid dendritic cells (PDC) and induced PDC apoptosis. Feb 25 2020
S2658 Omipalisib (GSK2126458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Phase 1. Feb 25 2020
S2794 Sofosbuvir (GS-7977) Sofosbuvir (PSI-7977, GS-7977) is a HCV NS5B polymerase inhibitor for the treatment of chronic hepatitis C virus (HCV) infection. Feb 25 2020
S7284 Rociletinib (CO-1686) Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively. Phase 2. Feb 25 2020
S7886 Onatasertib(CC 223) CC-223 is a potent, selective, and orally bioavailable mTOR inhibitor with IC50 of 16 nM, >200-fold selectivity over the related PI3K-α. Phase 1/2. Feb 25 2020
S2736 Fedratinib (TG101348) Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and Ret with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2. Feb 25 2020
S1147 Barasertib (AZD1152-HQPA) Barasertib (AZD1152-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1. Feb 25 2020
S7634 Cerdulatinib (PRT062070) Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM. Feb 25 2020
S1782 Azacitidine (5-Azacytidine) Azacitidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy. Feb 25 2020
S8455 Talabostat (PT-100) Talabostat (Val-boroPro, PT-100) is a dipeptidyl peptidase inhibitor with IC50 values of <4 nM, 4 nM, 11 nM, 310 nM, 560 nM and 390 nM for DPP-IV, DPP8, DPP9, QPP, FAP and PEP respectively. It has antineoplastic and hematopoiesis- stimulating activities. Feb 25 2020
S2811 Sapanisertib (MLN0128) Sapanisertib (INK 128, MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1. Feb 25 2020
S8048 Venetoclax (ABT-199) Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3. Feb 25 2020
S8397 Eltanexor(KPT-8602) Eltanexor(KPT-8602) is a second-generation, orally bioavailable XPO1 (also known as CRM1) inhibitor with IC50 values of 20−211 nM in 10 AML lines after 3 days exposure. Feb 25 2020
Cat.No. Product Name Information Added
S2247 Buparlisib (BKM120) Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2. Feb 25 2020
S2072 Seratrodast(AA-2414) Seratrodast is a potent and selective thromboxane A2 receptor (TP) antagonist with IC50 of 40 nM used primarily in the treatment of asthma and used as anti-inflammatory agent. Feb 25 2020
S7654 Defactinib (VS-6063) Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2. Feb 25 2020
S1222 Dexrazoxane HCl (ICRF-187) Dexrazoxane HCl (ICRF-187, ADR-529) is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II Feb 25 2020
S7173 Spebrutinib (CC-292) Spebrutinib (CC-292, AVL-292) is a covalent, orally active, and highly selective BTK inhibitor with IC50 of <0.5 nM, displaying at least 1400-fold selectivity over the other kinases assayed. Phase 1. Feb 25 2020
S8041 Cobimetinib (GDC-0973) Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3. Feb 25 2020
S8840 SEL120(SEL120-34A) hydrochloride SEL120(SEL120-34,SEL120-34A) is a novel inhibitor of Cyclin-dependent kinase 8 (CDK8) with IC50 values of 4.4 nM and 10.4 nM for CDK8/Cyclin C and CDK19/CyclinC respectively. Feb 25 2020
S5307 PSI-6206 (GS-331007) PSI-6206 (RO-2433, GS-331007) is a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase, targeting NS5B polymerase. Feb 25 2020
S8015 CEP-32496(RXDX-105) CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2. Feb 25 2020
S6753 CP 640186 CP 640186 is an isozyme-nonselective ACC (Acetyl-CoA carboxylase) inhibitor with IC50 values of 53 and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2, respectively. Feb 25 2020
S7111 IDO-IN-2 IDO-IN-2 (NLG-919 analogue) is a a potent IDO1 inhibitor with IC50 of 38 nM. Feb 25 2020
S7208 Bisindolylmaleimide I (GF109203X) Bisindolylmaleimide I (GF109203X) is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor. Feb 24 2020
S6657 2-Aminoethyl Diphenylborinate (2-APB) 2-Aminoethyl Diphenylborinate (2-APB) is an IP3 receptor inhibitor and regulate IP3-induced calcium release.2-APB also inhibits the SOC channel activity and activates TRP channel at higher concentrations. Feb 24 2020
S2638 NU7441 (KU-57788) NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage. Feb 24 2020
S5245 Raltegravir potassium Raltegravir Potassium is the orally bioavailable potassium salt of raltegravir, the first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor. Feb 24 2020
S8808 DC661 DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ). DC661 induces apoptosis. Feb 21 2020
S2934 Ensartinib (X-396) dihydrochloride Ensartinib (X-396) is a potent new-generation ALK inhibitor with high activity against a broad range of known crizotinib-resistant ALK mutations and CNS metastases. It potently inhibits both wild-type ALK and ALK variants (F1174, C1156Y, L1196M, S1206R, T1151, and G1202R mutants) with in vitro IC50s of <4 nM. Feb 21 2020
S6645 AZD5069 AZD5069 is a novel antagonist of CXCR2, which is shown to inhibit binding of CXCL8 to CXCR2 with a pIC50 value of 8.8 and inhibit CXCL8 binding to CXCR1 with pIC50 values of 6.5. Feb 21 2020
S5268 Solithromycin Solithromycin, belonging to the well-known class of macrolide antibiotics that also includes azithromycin, is a potent bacterial protein synthesis inhibitor. Feb 21 2020
S8708 AZD0364(ATG-017) AZD0364 is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2. Feb 21 2020
Cat.No. Product Name Information Added
S4504 6-Mercaptopurine (6-MP) Monohydrate 6-Mercaptopurine Monohydrate is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA. Feb 21 2020
S6086 2-Phenylbutyric acid 2-Phenylbutyric acid, belongs to the class of organic compounds known as phenylpropanes, is used as an anticholesteremic. Feb 21 2020
S6418 PF 429242 PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM, showing no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 μM and only modest inhibition of urokinase (IC50 = 50 μM) and factor Xa (IC50 = 100 μM). Feb 21 2020
S3680 NLRP3 Inflammasome Inhibitor I NLRP3 Inflammasome Inhibitor I, an intermediate substrate in the synthesis of glyburide which is free of the cyclohexylurea moiety involved in insulin release, is a novel inhibitor of the NLRP3 inflammasome. Feb 21 2020
S8720 AZD4635 (HTL1071) AZD4635 (HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors. Feb 21 2020
S5859 Sancycline Sancycline is a semi-synthetic tetracycline antibiotic. Feb 21 2020
S1166 Cisplatin Cisplatin is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy. Solutions are best fresh-prepared. Feb 18 2020
S6122 Cyclohexanecarboxamide Cyclohexanecarboxamide is a cooling agent and an agonist at TRPM8 receptors (EC50 = 3.7 μM). Feb 14 2020
S6638 AMG-333 AMG-333 is a potent and highly selective antagonist of TRPM8 with IC50 values of 13 nM and 30 nM for human TRPM8 and rat TRPM8. Feb 14 2020
S7999 SKF96365 SKF96365, originally identified as a blocker of receptor-mediated calcium entry, is widely used diagnostically, as a blocker of transient receptor potential canonical type (TRPC) channels. Feb 14 2020
S8691 ML204 ML204 is a novel, potent, and selective TRPC4 channel inhibitor with apparent IC50 values of about 1 μM in fluorescent intracellular Ca2+ assays and about 3 μM in whole-cell voltage clamp experiments. It exhibits some selectivity within the TRPC subfamily of channels and higher selectivity against other TRP channels and non-TRP channels. Feb 14 2020
S8073 Optovin Optovin is a reversible photoactivated TRPA1 activator. Feb 14 2020
S6637 HC-067047 HC-067047 is a selective TRPV4 channel antagonist with IC50 values of 48 nM,133 nM,and 17 nM for human, rat, and mouse TRPV4 orthologs,respectively. Feb 14 2020
S4022 Probenecid Probenecid is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16. Probenecid is also a clinically used broad-spectrum Pannexin1 (Panx1) blocker. Feb 14 2020
S7827 4-Hydroxytamoxifen(Afimoxifene) 4-Hydroxytamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants. Feb 14 2020
S8137 Capsazepine Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist. Feb 14 2020
S6669 MC-Val-Cit-PAB MC-Val-Cit-PAB,also known as MC-Val-Cit-PAB-OH,is a cathepsin cleavable ADC peptide linker and is used for making ADC conjugate (antibody-drug conjugate). Feb 14 2020
S6649 E7046(ER-886406) E7046 is a selective inhibitor of the prostaglandin E2 (PGE2) receptor EP4 with IC50 of 13.5 nM and Ki of 23.14 nM. Feb 14 2020
S8891 JHU-083 JHU-083 is a novel prodrug of DON.JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress.Solutions are best fresh-prepared. Feb 14 2020
S6634 SAR7334 SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels.SAR7334 blocks TRPC6 currents with an IC50 of 7.9 nM in patch-clamp experiment. Feb 14 2020
Cat.No. Product Name Information Added
S2773 SB705498 SB705498 is a TRPV1 antagonist for hTRPV1, antagonizes capsaicin, acid, and heat activation of TRPV1 with IC50 of 3 nM, 0.1 nM and 6 nM, shows a degree of voltage dependence, exhibits >100-fold selectivity for TRPV1 over TRPM8. Phase 2. Feb 14 2020
S9466 Methenamine Hippurate Methenamine Hippurate is the hippurate salt form of methenamine, a prodrug and inactive weak base that is hydrolyzed to formaldehyde in acid urine.Methenamine Hippurate is the component of Hiprex drug which has antibacterial activity. Feb 14 2020
S6409 Zucapsaicin Zucapsaicin, the cis-isomer of capsaicin, is a topical analgesic used to treat osteoarthritis of the knee and other neuropathic pain. It is also a TRPV-1 modulator. Feb 14 2020
S8367 GSK2193874 GSK2193874 is an orally active, potent, and selective blocker of transient receptor potential vanilloid 4 (TRPV4) with IC50 values of 0.04 and 0.002 μM for hTRPV4 and rTRPV4, respectively. Feb 14 2020
S6410 Clemizole Clemizole, a first-generation histamine receptor (H1) antagonist, is a potent inhibitor of behavioural and electrographic seizure activity. It has a potential therapeutic effect on hepatitis C infection and also potently inhibits TRPC5 ion channels. Feb 14 2020
S8107 GSK1016790A GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells. Feb 14 2020
S8238 SB366791 SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist with an IC50 of 5.7 nM. Feb 14 2020
S7115 AMG-517 AMG 517 is a potent and selective TRPV1 antagonist, and antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM, respectively. Feb 14 2020
S2918 HC-030031 HC-030031 is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx with IC50 of 6.2 μM and 5.3 μM respectively. Feb 14 2020
S4516 (+)-Camphor Camphor is a waxy, flammable, white or transparent solid with a strong aroma, often used to relieve pain, reduce itching and treat fungal infections. It can activate TRPV1 and TRPV3. Feb 14 2020
S8505 LY2510924 LY2510924 is a potent and selective CXCR4 antagonist that specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nmol/L and inhibits SDF-1-induced GTP binding with Kb value of 0.38 nmol/L. Feb 13 2020
S2700 KX2-391(Tirbanibulin) KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2. Feb 10 2020
S8728 PK11000 PK11000 stabilizes the DBD of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding and effective in inducing cell death. Feb 10 2020
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs). Feb 09 2020
S1378 Ruxolitinib (INCB018424) Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis. Feb 04 2020
S8501 Adaptavir (DAPTA) DAPTA is a water soluble potent, selective CCR5 antagonist which potently inhibits specific CD4-dependent binding of gp120 Bal (IC50 = 0.06 nM) and CM235 (IC50 = 0.32 nM) to CCR5. Feb 02 2020
S6666 FT113 FT113 is a potent inhibitor of fatty acid synthase (FAS/FASN) with ic50 of 213 nM. Jan 20 2020
S6667 STING inhibitor C-178 C-178 is a covalent inhibitor of STING,covalently bind to Cys91. Jan 20 2020
S8907 Dapansutrile (OLT1177) Dapansutrile (OLT1177) is a novel and selective NLRP3 inflammasome inhibitor. Jan 20 2020
S8909 UBCS039 UBCS039 is the first synthetic SIRT6 activator with EC50 of 38 μM,induces a time-dependent activation of autophagy in several human tumor cell lines. Jan 20 2020
Cat.No. Product Name Information Added
S6665 Sparsentan (PS-433540,RE-021,DARA) Sparsentan is a dual endothelin type A receptor(ETA) and angiotensin II type 1 receptor antagonist. Jan 20 2020
S6668 NVS-ZP7-4 NVS-ZP7-4,a Zinc transporter SLC39A7 (ZIP7) inhibitor,is the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway. Jan 20 2020
S6639 BAY-545 BAY-545 is an A2B adenosine receptor antagonist with ic50 of 59 nM. Jan 20 2020
S8559 INF39 INF39 is a nontoxic, irreversible NLRP3 inhibitor that counteracts NLRP3 activation through direct irreversible interaction with NLRP3 and partial inhibition of LPS-driven pro-inflammatory gene expression. Jan 19 2020
S5774 CY-09 CY-09 is a specific NLRP3 inflammasome inhibitor that directly targeted NLRP3 itself。 It is tested against the five major cytochrome P450 enzymes 1A2, 2C9, 2C19, 2D6, and 3A4 with half maximal inhibitory concentration (IC50) values of 18.9, 8.18, >50, >50, and 26.0 µM, respectively. Jan 19 2020
S7809 MCC950 Sodium (CP-456773 Sodium) MCC950 Sodium (CP-456773 Sodium) is a potent, selective inhibitor of NLRP3 with IC50 of 7.5 nM in BMDMs; but not the AIM2, NLRC4 or NLRP1 inflammasomes. Jan 19 2020
S1575 RO4929097 RO4929097 is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2. Jan 19 2020
S6662 AST-487 (NVP-AST487) AST-487,a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM. Jan 17 2020
S6660 B-Raf inhibitor 1 (Compound 13) dihydrochloride B-Raf inhibitor 1 (Compound 13) is a type IIA Raf inhibitor which bind to the DFG-out conformation with ki of 1 nM,1 nM,and 0.3 nM for B-Raf(WT), B-Raf(V600E) and C-Raf, respectively. Jan 17 2020
S4303 9-Aminoacridine 9-Aminoacridine is a highly fluorescent dye used clinically as a topical antiseptic and experimentally as a mutagen, an intracellular pH indicator and a negative mode small molecule MALDI matrix. Jan 17 2020
S4393 Cephapirin Sodium Cephapirin Sodium is the sodium salt form of cephapirin, a semi-synthetic, first-generation cephalosporin antibiotic with bactericidal activity.Cephapirin Sodium is effective against gram-negative and gram-positive organisms. Jan 17 2020
S4404 Pasiniazid Pasiniazid is a composition of isoniazid and 4-aminosalicylic acid, used to treat tuberculosis patients. Jan 17 2020
S4414 Sodium 4-aminohippurate Sodium 4-aminohippurate is a derivative of hippuric acid. Jan 17 2020
S8904 USP25/28 inhibitor AZ1 AZ1 is a potent and noncompetitive dual Inhibitors of the ubiquitin-specific protease (USP) 25/28 with IC50s of 0.62 μM and 0.7 μM in Ub-RH110 assay,respectively. Jan 16 2020
S6650 EN6 EN6 is a novel covalent autophagy activator and targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase with an IC50 of 1.7 μM for recombinant human ATP6V1A protein. Jan 16 2020
S7110 (+)-JQ1 (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. Jan 16 2020
S1214 Bleomycin Sulfate Bleomycin Sulfate is a glycopeptide antibiotic and an anticancer agent for squamous cell carcinomas (SCC) with IC50 of 4 nM in UT-SCC-19A cells. Jan 16 2020
S8503 BLU-554 (BLU554/Fisogatinib) BLU-554 is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM. Jan 15 2020
S1215 Carboplatin Carboplatin is a DNA synthesis inhibitor by binding to DNA and interfering with the cell's repair mechanism in A2780, SKOV-3, IGROV-1, and HX62 cells. Solutions are best fresh-prepared. Jan 15 2020
S1014 Bosutinib (SKI-606) Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy. Jan 14 2020
Cat.No. Product Name Information Added
S8895 Ziritaxestat (GLPG1690) Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM. Jan 14 2020
S8868 NG25 NG25 is a novel inhibitor of TAK1 with enzymatic IC50s of 149 and 21.7 nM for TAK1 and MAP4K2 respectively. Jan 14 2020
S8663 Takinib Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Jan 14 2020
S6755 NS 11394 NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes. Jan 14 2020
S6563 DMNQ DMNQ is a 1,4-naphthoquinone that acts as a redox-cycling agent, typically increasing intracellular superoxide and hydrogen peroxide formation. Jan 10 2020
S6654 SRI-011381 SRI-011381 is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease. Jan 09 2020
S8785 A1874 A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency. Jan 09 2020
S8899 FF-10101 FF-10101 is a novel irreversible FLT3 inhibitor with ic50 of 0.20 nM and 0.16 nM for FLT3 (WT) and FLT3(D835Y), respectively. Jan 09 2020
S6647 Bardoxolone Bardoxolone,acts by releasing Nrf2 from KEAP1,is a highly potent activator of Nrf2 that induce programmed cell death (apoptosis) in cancer cells. Jan 09 2020
S6651 G15 (GRB-G15) G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM. Jan 09 2020
S6656 VAS2870 VAS2870 is a pan-NADPH oxidase (NOX) inhibitor. Jan 09 2020
S8882 ODM-203 ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively. Jan 09 2020
S6652 H-151 H-151 is a highly potent and covalent antagonist of STING that has noteworthy inhibitory activity both in human cells and in vivo. Jan 08 2020
S8880 Lobaplatin ( D-19466) Lobaplatin (D-19466) is a third-generation platinum anti-neoplastic agent. It is a platinum complex with DNA alkylating activity. Jan 08 2020
S3734 Albiglutide Fragment Albiglutide fragment is one copy of a 30-amino-acid sequence of modified human GLP-1 (fragment 7-36). Jan 07 2020
S8037 Necrostatin-1 Necrostatin-1 is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis. Jan 07 2020
S7242 Erastin Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. Jan 07 2020
S7786 Erlotinib Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy. Jan 07 2020
S7243 Ferrostatin-1 (Fer-1) Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM. Jan 07 2020
S7397 Sorafenib Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. Jan 07 2020
Cat.No. Product Name Information Added
S7699 Liproxstatin-1 Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM. Jan 07 2020
S1413 Bafilomycin A1(Baf-A1) Bafilomycin A1 is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis. Jan 07 2020
S7079 SGC 0946 SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM in a cell-free assay, is inactive against a panel of 12 PMTs and DNMT1. Jan 07 2020
S1148 Docetaxel Docetaxel, an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules. Jan 07 2020
S8155 RSL3 RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS. RSL3 binds, inactivates GPX4 and thus mediates GPX4-regulated ferroptosis. Jan 07 2020
S7023 Z-VAD-FMK Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells. Jan 07 2020
S2619 MG-132 MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 μM and 1.2 μM for the inhibition of proteasome and calpain, respectively. MG132 activates autophagy and induces apoptosis in tumor cells. Jan 07 2020
S6719 E6446 (dihydrochloride) E6446 is a specific Toll-like receptor 9 inhibitor. Jan 07 2020
S1029 Lenalidomide (CC-5013) Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Jan 06 2020
S1623 Acetylcysteine(N-acetylcysteine) Acetylcysteine(N-acetyl-l-cysteine) is a ROS(reactive oxygen species) inhibitor that antagonizes the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor. Acetylcysteine(N-acetyl-l-cysteine) suppresses TNF-induced NF-κB activation through inhibition of IκB kinases. Acetylcysteine(N-acetyl-l-cysteine) induces apoptosis via the mitochondria-dependent pathway. Acetylcysteine(N-acetyl-l-cysteine) inhibits ferroptosis and virus replication.Solutions of Acetylcysteine are best fresh-prepared. Jan 06 2020
S7678 Sacubitril/valsartan (LCZ696) Sacubitril/valsartan (LCZ696), consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3. Jan 06 2020
S8278 SHP099 HCl SHP099 is a highly potent, selective and orally bioavailable small-molecule SHP2 inhibitor with an IC50 value of 0.071 μM and shows no activity against SHP1. Jan 06 2020
S2916 ML161(Parmodulin 2) ML-161 is an allosteric inhibitor of PAR1 with IC50 of 0.26 μM. Jan 06 2020
S7171 Setanaxib (GKT137831) GKT137831 is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectivelyl; ~10-fold selectivity towards NOX1, 4 and 5 over NOX2, does not inhibit XO or scavange ROS/RNS. Jan 06 2020
S6170 Benzyldodecyldimethylammonium Chloride Dihydrate Benzyldodecyldimethylammonium Chloride Dihydrate is a chemical. Jan 06 2020
S7833 OICR-9429 OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro. It binds to WDR5 with high affinity (KD = 93 ± 28 nM. Jan 03 2020
S8444 KPT 9274( ATG-019) KPT-9274 is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay. Jan 03 2020
S6575 C-176 (STING inhibitor) STING inhibitor C-176 is a potent, small-molecule inhibitor of STING, a central signaling component of the intracellular DNA sensing pathway. Jan 03 2020
S2627 Tubastatin A HCl Tubastatin A HCl is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Jan 03 2020
S8796 diABZI STING agonist(compound 3) STING agonist 1 (compound 3) is a potent non-nucleotide STING agonist and has tremendous potential to improve treatment of cancer in humans. Jan 03 2020
Cat.No. Product Name Information Added
S6747 SW-044248 SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells. Jan 02 2020
S8901 DS-6051b DS-6051b is a new-generation selective ROS1/NTRK inhibitor with ic50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM for ROS1,NTRK1,NTRK2 and NTRK3,respectively. Jan 02 2020
S8847 BAY 2402234 BAY 2402234 is a novel and selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 1.2 nM. Jan 02 2020
S6636 Azaindole 1 (TC-S 7001) Azaindole 1 (TC-S 7001) is a selective Rho-associated protein kinase (ROCK) inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2 in an ATP-competitive manner. Jan 02 2020
S6655 WM-8014 WM-8014 is a highly potent inhibitor of histone acetyltransferase KAT6A with an IC50 of 8 nM. Jan 02 2020
S8878 NDI-091143 NDI-091143 is a potent inhibitor of human ATP-citrate lyase(ACLY) with a Ki of 7.0 nM and an IC50 of 2.1 nM in the ADP-Glo assay. Jan 02 2020
S5650 Sodium Hyaluronate Sodium hyaluronate is the sodium salt of hyaluronic acid, a glycosaminoglycan found in various connective tissue of humans. Jan 02 2020
S1142 Alvespimycin (17-DMAG) HCl Alvespimycin (17-DMAG) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2. Jan 02 2020
S7933 VR23 VR23 is a potent proteasome inhibitor with IC50 of 1 nM, 50-100 nM, and 3 μM for trypsin-like proteasomes, chymotrypsin-like proteasomes, and caspase-like proteasomes, respectively. Dec 31 2019
S2929 Pifithrin-α (PFTα) HBr Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR). Dec 31 2019
S1950 Metformin HCl Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153. Dec 30 2019
S4592 Captisol (SBE-β-CD) Captisol (SBE-β-CD) is a novel, chemically modified cyclodextrin with a structure designed to optimize the solubility and stability of drugs. Dec 30 2019
S7753 BPTES BPTES is a potent and selective Glutaminase GLS1 (KGA) inhibitor with IC50 of 0.16 μM. It has no effect on glutamate dehydrogenase activity and causes only a very slight inhibition of γ-glutamyl transpeptidase activity. Dec 30 2019
S2226 Idelalisib (CAL-101, GS-1101) Idelalisib (CAL-101, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy. Dec 30 2019
S1006 Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3. Dec 29 2019
S5001 Tofacitinib (CP-690550) Citrate Tofacitinib citrate (CP-690550 citrate) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively. Tofacitinib citrate has anti-infection activity. Dec 29 2019
S7306 Dorsomorphin (Compound C) 2HCl Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line. Dec 29 2019
S1030 Panobinostat (LBH589) Panobinostat (LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3. Dec 29 2019
S1036 PD0325901(Mirdametinib) PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 2. Dec 29 2019
S1039 Rapamycin (Sirolimus) Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells. Dec 29 2019
Cat.No. Product Name Information Added
S1068 Crizotinib (PF-02341066) Crizotinib (PF-02341066) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. Dec 29 2019
S1105 LY294002 LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis. Dec 29 2019
S2215 DAPT (GSI-IX) DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy. Dec 29 2019
S1144 Ivacaftor (VX-770) Ivacaftor (VX-770) is a selective potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM in fisher rat thyroid cells, respectively. Dec 29 2019
S2673 Trametinib (GSK1120212) Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. Trametinib activates autophagy and induces apoptosis. Dec 29 2019
S2680 Ibrutinib (PCI-32765) Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc. Ibrutinib is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I. Dec 29 2019
S1250 Enzalutamide (MDV3100) Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy. Dec 29 2019
S1263 CHIR-99021 (CT99021) CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy. Dec 29 2019
S8606 HDM201 (Siremadlin) HDM201 is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4. Dec 27 2019
S1696 Hydrocortisone (cortisol) Hydrocortisone (cortisol) is a steroid hormone or glucocorticoid produced by the adrenal gland. Dec 26 2019
S7033 GSK2656157 GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases. Dec 25 2019
S7693 AZD6738(Ceralasertib) AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2. Dec 24 2019
S7655 CB-839(Telaglenastat) CB-839(Telaglenastat) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1. Dec 24 2019
S8322 LY3023414(Samotolisib) LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK. Dec 24 2019
S8199 LTX-315(Ruxotemitide) LTX-315 is the oncolytic peptide that kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization. Dec 24 2019
S6227 Acrylamide monomer Acrylamide is a neurotoxic monomer with extensive industrial applications. It could be used as a precursor to polyacrylamides. Dec 24 2019
S7297 Osimertinib (AZD9291) Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3. Dec 22 2019
S5543 1, 10-Phenanthroline monohydrate 1,10-Phenanthroline is a classic chelating bidentate ligand for transition metal ions that has played an important role in the development of coordination chemistry. It is an inhibitor of metallopeptidases. Dec 22 2019
S6628 E7820 E7820 is a unique angiogenesis inhibitor with antitumor activities. Dec 20 2019
S9519 Fadrozole Fadrozole is a potent, selective, nonsteroidal inhibitor of aromatase with an IC50 of 4.5 nM and selectivity over other cytochrome P-450 enzymes. Dec 20 2019
Cat.No. Product Name Information Added
S2717 CP-91149 CP-91149 is a selective glycogen phosphorylase (GP) inhibitor with IC50 of 0.13 μM in the presence of glucose, 5- to 10-fold less potent in the absence of glucose. Dec 20 2019
S6648 PF-06282999 PF-06282999 is an orally bioavailable, irreversible inactivator of myeloperoxidase enzyme and is currently in clinical trials for the potential treatment of cardiovascular diseases. Dec 19 2019
P1089 Goserelin Acetate Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 1 nM. Dec 19 2019
S9521 Pentostatin Pentostatin is a potent inhibitor of adenosine deaminase. The drug is effective in the treatment of many lymphoproliferative malignancies, particularly hairy-cell leukemia. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity. Dec 19 2019
S6646 CPI-444 CPI-444 is a potent and selective Adenosine A2A receptor antagonist. It binds to A2A receptors with a Ki of 3.54 nmol/L and demonstrates a greater than 50-fold selectivity for the A2A receptor over other adenosine receptor subtypes. Dec 19 2019
S9522 Valrubicin Valrubicin is a chemotherapy drug used to treat bladder cancer. Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively. Dec 19 2019
S9520 Lasofoxifene Tartrate Lasofoxifene Tartrate is a third-generation, non-steroidal selective estrogen receptor modulator (SERM) which binds with high affinity to the human estrogen receptor-α with IC50 value of 1.5 nM. Dec 19 2019
S6633 AM 095 AM095 is an antagonist of the LPA type 1 receptor with IC50 values of 0.98 and 0.73 μM for recombinant human and mouse LPA1, respectively. Dec 19 2019
S5712 Zofenopril calcium Zofenopril calcium is an angiotensin-converting enzyme (ACE) inhibitor that protects the heart and helps reduce high blood pressure. Dec 19 2019
S1146 Cyclopamine Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells. Dec 19 2019
S4345 Pentoxifylline Pentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity. Dec 19 2019
S4353 Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9. Dec 19 2019
S8848 Futibatinib (TAS-120) Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 3.9 nM, 1.3 nM, 1.6 nM and 8.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4 respectively. Dec 19 2019
S4357 Tacrine HCl Tacrine is a centrally acting anticholinesterase and indirect cholinergic agonist. Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively. Dec 19 2019
S4360 Tolmetin Sodium Tolmetin is a non-steroidal anti-inflammatory drug of the arylalkanoic acids. Tolmetin sodium dihydrate is a non-steroidal antiinflammatory agent, and acts as a non-selective COX inhibitor. Dec 19 2019
S4368 Carbenoxolone Sodium Carbenoxolone, a synthetic derivative of glycyrrhetinic acid, is also used as a blocker of the enzyme 11β-hydroxysteroid dehydrogenase (11β-HSD), of pannexon membrane channels (comprising 6 subunits of pannexin) and the related innexon channels. Dec 19 2019
S4377 Imipramine HCl Imipramine is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination). Dec 19 2019
S4382 Pyrilamine Maleate Pyrilamine is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling. Dec 19 2019
S6643 R-7050 R-7050 is a cell permeable TNF-α receptor antagonist and is 2.3-fold more selective for TNF-α-mediated signaling than for that driven by IL-1β. Dec 16 2019
S6642 Branaplam (LMI070) Branaplam (LMI070) is a highly selective, small-molecule splicing modulators of survival motor neuron‑2 (SMN2) with an EC50 of 0.02 μM. Dec 16 2019
Cat.No. Product Name Information Added
S8839 Borussertib Borussertib is a covalent-allosteric inhibitor of protein kinase Akt with an IC50 of 0.8 nM and a Ki of 2.2 nM for WT Akt. Dec 16 2019
S5631 L-Alanine Alanine is a naturally occuring non-essential amino acid that is involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brainR, and the CNS. Dec 15 2019
S5629 L-Proline L-Proline is one of non-essential amino acids and an essential component of collagen that is important for proper functioning of joints and tendons. Dec 15 2019
S5630 L-lysine Lysine is an α-amino acid that is used in the biosynthesis of proteins and is required for growth and tissue repair. Dec 15 2019
S5634 L-arginine Arginine is an important amino acid used in the biosynthesis of proteins. L-arginine plays an important role in immune regulation by affecting the immune response and inflammation. It is also implicated in cell division, wound healing and the release of hormones. Dec 15 2019
S5633 L-methionine L-Methionine is an essential sulfur-containing, free-form amino acid, acts as an antioxidant promoter, and contributes to the synthesis of S-adenosyl-L-methionine (SAMe). Dec 15 2019
S7060 PP1 PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM. Dec 11 2019
S1048 Tozasertib (VX-680, MK-0457) Tozasertib (VX-680, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. Phase 2. Dec 11 2019
S1077 SB202190 (FHPI) SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis. Dec 11 2019
S7774 SU6656 SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively. Dec 11 2019
S1100 MLN8054 MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1. Dec 11 2019
S1109 BI 2536 BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2. Dec 11 2019
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3. Dec 11 2019
S1574 Doramapimod (BIRB 796) Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2. Dec 11 2019
S7917 Kenpaullone Kenpaullone is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It also inhibit glycogen synthase kinase 3β (GSK3β) with IC50 of 0.23 µM. Dec 11 2019
S1145 SNS-032 (BMS-387032) SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. Phase 1. Dec 11 2019
S7152 C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. Dec 11 2019
S2843 BI-D1870 BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. Dec 11 2019
S8206 Ivosidenib (AG-120) Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Dec 10 2019
S2807 Dabrafenib (GSK2118436) Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively. Dec 10 2019
Cat.No. Product Name Information Added
S6740 DB07268 DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM and exhibits at least 70- to 90-fold greater potency against JNK1 than CHK1, CK2, and PLK. Dec 09 2019
S6623 APY29 APY29 is a type I kinase inhibitor of IRE1α that binds to the ATP-binding site on IRE1α and inhibits its autophosphorylation (IC50 = 280 nM) and enhances its RNase function (EC50 = 460 nM). Dec 09 2019
S6625 Temsavir (BMS-626529) Temsavir (BMS-626529) is a novel small-molecule HIV-1 attachment inhibitor active against both CCR5- and CXCR4-tropic viruses. Dec 09 2019
S6751 Brevianamide F Brevianamide F, belonging to a class of naturally occurring 2,5-diketopiperazines, is the simplest member and the biosynthetic precursor of a large family of biologically active prenylated tryptophan-proline 2,5-diketopiperazines that are produced by the fungi A.fumigates and Aspergillus sp.. Dec 09 2019
S6749 ASP-9521 ASP-9521 is a selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase type 5 (17β-HSD5). Dec 09 2019
S6739 MN 64 MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively. Dec 09 2019
S6746 APD668 APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively. Dec 09 2019
S6632 Mirogabalin (DS-5565) Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand that has been used in trials studying the treatment of Post-herpetic Neuralgia, Pain Associated With Fibromyalgia, and Diabetic peripheral neuropathic pain. Dec 09 2019
S6629 GNE-617 GNE-617 is a highly potent inhibitor of NAMPT activity with an IC50 of 5 nM. Dec 09 2019
S6644 Radiprodil (RGH-896) Radiprodil (RGH-896) is a NR2B-selective NMDA receptor antagonist, initially developed for the treatment of neuropathic pain. Dec 09 2019
S6624 Avatrombopag Avatrombopag is an orally administered, small-molecule thrombopoietin receptor (c-Mpl) agonist which increases platelet number, but not platelet activation. Dec 09 2019
S8820 PTC596 PTC596 is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. It inhibits cell proliferation and induces apoptosis in a dose- and time-dependent manner. IC50 values at 72 hours ranged from 68 to 340 nM in mantle cell lymphoma (MCL) cell lines. Dec 09 2019
S7673 L-685,458 L-685,458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM. Dec 09 2019
S6631 Belotecan (CKD-602) hydrochloride Belotecan (CKD-602) is a potent DNA topoisomerase I inhibitor that exerts a clinical anticancer effect on various types of tumor. Dec 09 2019
S6741 SB-756050 SB-756050 is a selective TGR5 agonist (EC50 = 1.3 μM for the human receptor). Dec 09 2019
S6744 Inauhzin Inauhzin is a cell-permeable SIRT1 inhibitor with an IC50 of 0.7-2 μM and reactivates p53 by inhibiting SIRT1 deacetylation activity. Dec 09 2019
S6737 C7280948 C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro. Dec 09 2019
S6728 IDO-IN-1 IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 59 nM. Dec 09 2019
S6758 I-CBP112 I-CBP112 is a potent and selective CBP/p300 inhibitor with dissociation constant (KD) of 151 ± 6 nM and 167 ± 8 nM for CBP and p300, respectively. Dec 09 2019
S6752 Y16 Y16 is an inhibitor of G-protein-coupled Rho GEFs. It blocks the binding of LARG, a DBL-family Rho guanine nucleotide exchange factor, with Rho (Kd = 80 nM). Dec 09 2019
Cat.No. Product Name Information Added
S4115 Hydroxypropyl Cellulose Hydroxypropyl cellulose (HPC) is a derivative of cellulose with both water solubility and organic solubility, it is used as food additive and sieving matrix for DNA separations. Dec 05 2019
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. Dec 05 2019
S1346 Heparin sodium Heparin sodium, a sulfated polysaccharide belonging to the family of glycosaminoglycans, has numerous important biological activities associated with its interaction with diverse proteins, used as an anticoagulant. Dec 05 2019
S6359 Purine Purine is a heterocyclic aromatic organic compound which plays crucial roles in DNA and RNA. It is also significant components in a number of other important biomolecules, such as ATP, GTP, cyclic AMP, NADH, and coenzyme A. Dec 05 2019
S2305 Grape Seed Extract Grape Seed Extract are industrial derivatives from whole grape seeds that have a great concentration of vitamin E, flavonoids, linoleic acid, and OPCs. Dec 05 2019
S1143 AG-490 (Tyrphostin B42) AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src. Dec 05 2019
S2609 Inulin Inulin(Inulin and sodium chloride), a starch found in the tubers and roots of many plants. Since it is hydrolyzable to fructose, it is classified as a fructosan. Dec 05 2019
S6732 7ACC2 7ACC2 is a potent inhibitor of mitochondrial pyruvate transport 1 (MCT1) with an IC50 value of 10 nM for lactate uptake in SiHa human cervix carcinoma cells. Dec 05 2019
S6754 S1RA S1RA is a selective sigma-1 receptor (σ1R) antagonist with a reported binding affinity of Ki = 17.0 ± 7.0 nM for human σ1 receptor , selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels. Dec 05 2019
S6742 Etofenamate Etofenamate is a nonsteroidal anti-inflammatory drug (NSAID) used for the treatment of joint and muscular pain. Dec 05 2019
S6748 ML364 ML364 is a small molecule inhibitor of the deubiquitinase USP2 with an IC50 of 1.1 μM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate. Dec 05 2019
S6745 JW55 JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). Dec 05 2019
S6756 Siramesine HCl Siramesine is a sigma receptor agonist, selective for the σ2 subtype with IC50 values of 0.12 nM and 17 nM for σ2 and σ1 receptors respectively. Dec 05 2019
S6626 Brequinar Brequinar is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro. Dec 05 2019
S6627 E-4031 dihydrochloride E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type. Dec 05 2019
S1799 Ranolazine Ranolazine is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina. Dec 04 2019
S7724 APR-246 (PRIMA-1MET) APR-246, also known as PRIMA-1MET, is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. Nov 29 2019
S1238 Tamoxifen Tamoxifen is an antagonist of the estrogen receptor in breast tissue. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis. Nov 29 2019
S4252 Mechlorethamine HCl Mechlorethamine is the prototype of alkylating agents, it works by binding to DNA, crosslinking two strands and preventing cell duplication. Nov 27 2019
S5287 Tiletamine Hydrochloride Tiletamine is a lipophilc and potent vetrinary anesthetic. It is also a NMDA receptor antagonist. Nov 27 2019
Cat.No. Product Name Information Added
S2679 Flavopiridol HCl Flavopiridol HCl competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2. Nov 27 2019
S1224 Oxaliplatin Oxaliplatin is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells. DMF is recommended for dissolution. Solutions are best fresh-prepared. Nov 27 2019
S8605 C188-9 C188-9 is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors. Nov 27 2019
S2697 A-769662 A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity. Nov 27 2019
S4732 MPTP hydrochloride MPTP hydrochloride is a dopaminergic neurotoxin and cause selective destruction of dopaminergic neurons in animal models of parkinsonism. MPTP hydrochloride induces apoptosis. Nov 26 2019
S6083 DL-Dopa DL-Dopa is an immediate precursor of dopamine. Nov 26 2019
S2168 PD128907 HCl PD 128907 HCl is a potent and selective dopamine D3 receptor agonist, with EC50 of 0.64 nM, exhibits 53-fold selectivity over dopamine D2 receptor. Nov 26 2019
S7482 EHT 1864 2HCl EHT 1864 2HCl is a potent Rac family GTPase inhibitor with Kd of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. Nov 26 2019
S7143 LGK-974 LGK-974 is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM in TM3 cells. Phase 1. Nov 26 2019
S6479 Isohomovanillic acid Isohomovanillic acid is a deaminated metabolite of catecholamines formed by the enzyme catechol-O-methyltransferase which catalyzes the transfer of a methyl group from S-adenosylmethionine to catecholamines, including the neurotransmitters dopamine, epinephrine, and norepinephrine. Nov 26 2019
S5639 3,4-Dihydroxyphenylacetic acid 3,4-Dihydroxyphenylacetic acid (DOPAC) is a metabolite of the neurotransmitter dopamine. It modulates the aldehyde dehydrogenase (ALDH) activity and protects the cells from the acetaldehyde-induced cytotoxicity in vitro. Nov 26 2019
S1092 KU-55933 (ATM Kinase Inhibitor) KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy. Nov 25 2019
S3937 Pterostilbene Pterostilbene is a natural dietary compound and the primary antioxidant component of blueberries. It has been implicated in anticarcinogenesis, modulation of neurological disease, anti-inflammation, attenuation of vascular disease, and amelioration of diabetes. Nov 25 2019
P1020 Argpressin Acetate Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 1 nM. Nov 25 2019
P1027 Melanotan II Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 1 nM. Nov 25 2019
P1036 Thymosin β4 Acetate (0.95) Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 1 nM. Nov 25 2019
S5388 Betrixaban Betrixaban is a new, long-acting, oral and selective Factor Xa inhibitor that decreases prothrombinase activity and thrombin generation. Nov 25 2019
S5389 Betrixaban maleate Betrixaban maleate is the maleate salt form of Betrixaban, which is a Factor Xa inhibitor that decreases prothrombinase activity and thrombin generation. Nov 25 2019
P1047 Felypressin Acetate Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 1 nM. Nov 25 2019
S2820 TAE226 (NVP-TAE226) TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met. Nov 24 2019
Cat.No. Product Name Information Added
S3052 Rupatadine Fumarate Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively. Nov 22 2019
S4519 Citric acid trilithium salt tetrahydrate Citric acid trilithium salt tetrahydrate is a pharmaceutical and construction material. It is commonly used in HPLC gradient elution for quantification of amino acids. Nov 22 2019
S8716 Pralsetinib (BLU-667) Pralsetinib (BLU-667) is a highly potent and selective RET inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T). Nov 21 2019
S7417 Puromycin 2HCl Puromycin 2HCl is an aminonucleoside antibiotic, which acts as a protein synthesis inhibitor. Nov 21 2019
S8814 TAS6417 TAS6417 is a novel EGFR inhibitor that targets EGFR exon 20 insertion mutations while sparing wild-type (WT) EGFR. IC50 values ranges from 1.1 ± 0.1 to 8.0 ± 1.1 nmol/L. Nov 21 2019
S8861 Mavacamten (MYK-461) Mavacamten (MYK-461) is a small-molecule modulator of cardiac myosin that targets the underlying sarcomere hypercontractility of hypertrophic cardiomyopathy (HCM), one of the most prevalent heritable cardiovascular disorders. Nov 21 2019
S7419 Blasticidin S HCl Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes, and acts as a DNA and protein synthesis inhibitor, used to select transfected cells carrying bsr or BSD resistance genes. Nov 21 2019
S2796 WP1066 WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. Phase 1. Nov 20 2019
S6702 Tween 80 Tween 80 is a widely used non-ionic emulsifier that is added to cosmetics, pharmaceuticals, and foods. Nov 20 2019
S7980 VPS34-IN1 Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy. Nov 20 2019
S4244 Serotonin HCl Serotonin HCl is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist. Nov 20 2019
S6408 Hexetidine Hexetidine is an anti-bacterial and anti-fungal agent with local anesthetic, astringent, deodorant and antiplaque activity. Nov 18 2019
S8126 MK571 MK-571 is a selective, orally active CysLT1 receptor(Cysteinyl leukotriene receptor) antagonist. Nov 17 2019
S8205 Enasidenib (AG-221) Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme. Nov 17 2019
S7725 BLZ945 BLZ945 is an orally active, potent and selective CSF-1R inhibitor with IC50 of 1 nM, >1000-fold selective against its closest receptor tyrosine kinase homologs. Nov 17 2019
S8044 BMS-345541 BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM in cell-free assays, respectively. Nov 17 2019
S7334 ERK5-IN-1 ERK5-IN-1 is a potent, and selective ERK5 inhibitor with IC50 of 162 nM. Nov 15 2019
S6715 YHO-13177 YHO-13177, a novel acrylonitrile derivative, is a potent BCRP inhibitor. Nov 14 2019
S6596 AG-126 AG126 is a tyrosine kinase inhibitor which selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM. Nov 14 2019
S1314 Zoledronic Acid Zoledronic acid (ZA), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Nov 13 2019
Cat.No. Product Name Information Added
S6475 Polaprezinc Polaprezinc is an orally bioavailable chelate composed of zinc and L-carnosine, with potential gastroprotective, anti-oxidant, anti-ulcer and anti-inflammatory activities. Nov 13 2019
S2924 CHIR-99021 (CT99021) HCl CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins. Nov 13 2019
S8506 SCH-527123 SCH-527123 is a potent, orally bioavailable CXCR2/CXCR1 antagonist with IC50 values of 2.6 nM and 36 nM, respectively. Nov 13 2019
S6717 TCS-OX2-29 TCX-OX2-29 is a OX2R antagonist (pKi = 7.5) that exhibits >250-fold selectivity for hOX2R compared with hOX1R (IC50s = 40 nM and >10,000 nM, respectively). Nov 13 2019
S8874 PLX5622 PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3. Nov 12 2019
S1524 AT7519 AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2. Nov 11 2019
S3669 Carmustine Carmustine is a cell-cycle phase nonspecific alkylating antineoplastic agent and used in the treatment of brain tumors and various other malignant neoplasms. Nov 11 2019
S2711 Dibenzazepine (YO-01027) Dibenzazepine (YO-01027) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM in cell-free assays for APPL and Notch cleavage, respectively. Nov 11 2019
S7315 PFI-3 PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains. Nov 07 2019
S7521 Afuresertib (GSK2110183) Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2. Nov 07 2019
S8535 ABBV-2222 (GLPG2222) ABBV-2222 is a CFTR corrector studied for the treatment of cystic fibrosis (CF). Nov 07 2019
S6731 Eliprodil (SL-820715) Eliprodil (SL-820715) is a non-competitive NR2B-selective NMDA antagonist with IC50 value of 1 μM and is less potent for NR2A- and NR2C-containing receptors with IC50 > 100 μM. Nov 07 2019
S6735 JD-5037 JD-5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker with an IC50 value of 2 nM for CB1 receptor and > 1000 nM for CB2 receptor. Nov 07 2019
S6727 AX-024 HCl AX-024 blocks the interaction of the CD3ε PRS with SH3.1(Nck). Nov 07 2019
S6713 ITD-1 ITD-1 is a potent TGF-β inhibitor. It does not block the kinase activity of either type I (TGFBR1) or type II (TGFBR2) TGFβ receptors but potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2, and only minimally in response to Activin A. Nov 07 2019
S6716 NSC 185058 NSC185058 inhibits ATG4B, the lipidation of LC3B, and autophagy without affecting the MTOR or PtdIns3K pathways. Nov 07 2019
S6711 IQ-1S IQ-1S is a JNK3 inhibitor with Kd values of 87, 360 and 390 nM for JNK3, JNK2 and JNK1, respectively. Nov 07 2019
S6710 SGC-GAK-1 SGC-GAK-1 is a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK) with Ki value of 3.1 nM and >50-fold selectivity over nearest kinase. Nov 07 2019
S6712 S107 S107 is a Type 1 ryanodine receptor (RyR1) stabilizer that binds RyR1 and enhances the binding affinity of calstabin-1. Nov 07 2019
S6718 MKT-077 MKT-077 is a newly synthesized, highly water-soluble rhodacyanine dye that exhibits significant antitumor activity in a variety of model systems. Nov 07 2019
Cat.No. Product Name Information Added
S6721 JG98 JG-98 is an allosteric inhibitor of Hsp70 that binds tightly to a deep pocket that is conserved in members of the Hsp70 family. Nov 07 2019
S6599 KM11060 KM11060 is a small molecule that corrects the processing of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation. Nov 07 2019
S6595 THZ531 THZ531 is a selective covalent inhibitor of CDK12 and CDK13 with IC50 values of 158 and 69 nM, respectively. Nov 07 2019
S6723 LXS-196 LXS-196 is a selective inhibitor of protein kinase C (PKC). Nov 07 2019
S6622 BMS309403 BMS309403 is a small-molecule FABP4 inhibitor with nM affinity (Kd=4 nM for FABP4) and >100-fold selectivity against FABP5 as well as the heart isoform FABP3. Nov 07 2019
S2933 AM580 AM580 is a retinoic acid receptor agonist with Kd values of 8 nM, 131 nM and 450 nM for RARα, RARβ and RARγ. Nov 07 2019
S6714 INH14 INH14 is an inhibitor of TLR2-mediated NF-kB activation with IC50 values of 8.975 μM and 3.598 μM for IKKα and IKKβ, respectively. Nov 07 2019
S7077 Cilengitide trifluoroacetate Cilengitide is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2. Nov 05 2019
S1070 PHA-665752 PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM in cell-free assays, >50-fold selectivity for c-Met than RTKs or STKs. Nov 05 2019
S7170 RO5126766 (CH5126766) RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM,19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1. Nov 05 2019
S7013 Guadecitabine (SGI-110) Guadecitabine (SGI-110) is a next-generation hypomethylating agent whose active metabolite decitabine has a longer in-vivo exposure time than intravenous decitabine. Nov 04 2019
S1095 Dacinostat (LAQ824) Dacinostat (LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter. Nov 04 2019
S6726 MK1064 MK1064 is a selective orexin 2 receptor antagonist (2-SORA) with an IC50 of 18 nM. Nov 04 2019
S6725 PCI 29732 PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM. Nov 04 2019
S8843 AZD7648 AZD7648 is a potent inhibitor of DNA-PK with an IC50 of 0.6 nM in biochemical assay and more than 100-fold selective against 396 other kinases. Nov 04 2019
S6733 Edonerpic maleate Edonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ). Nov 04 2019
S6729 Besifovir Besifovir is novel and potent acyclic nucleotide phosphonate used to treat hepatitis B virus (HBV) infection. Nov 04 2019
S6730 CC-401 Hydrochloride CC-401 is a potent inhibitor of JNK with at least 40-fold selectivity against other related kinases. Nov 04 2019
S6616 ETC-159 ETC-159 is an orally available, potent porcupine inhibitor with an IC50 of 2.9 nM for inhibiting β-catenin reporter activity in STF3A cells. Nov 04 2019
S6617 MSX-122 MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM). Nov 04 2019
Cat.No. Product Name Information Added
S6619 ABT 702 dihydrochloride ABT-702 is a novel, potent non-nucleoside Adenosine kinase inhibitor with an IC50 of 1.7 nM. It has oral activity in animal models of pain and inflammation. Nov 04 2019
S8774 DT-061(SMAP) DT-061(SMAP) is a bioavailable PP2A activator. It decreases cell viability in HCC827 and HCC3255 cell lines, with IC50 values of 14.3 μM and 12.4 μM respectively. Nov 04 2019
S8681 ASTX660 ASTX660 is a potent, non-peptidomimetic antagonist of cIAP1/2 and XIAP that inhibits the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively. Nov 04 2019
S8710 LSZ102 LSZ102 is a potent, orally bioavailable selective estrogen receptor degrader that inhibits ERα transcription with an IC50 of 6 nM. Nov 04 2019
S8758 VU661013 VU661013 is a novel, potent, selective MCL1 inhibitor which exhibits a Ki of 97 ± 30 pM to human MCL-1 in a TR-FRET assay. However, VU661013 does not significantly inhibit BCL-xL (Ki > 40 μM) or BCL-2 (Ki = 0.73 μM). Nov 04 2019
S8257 CFI-402257 CFI-402257 is a potent highly selective, and orally active small-molecule inhibitor of Mps1 with Ki value of 0.09 ± 0.02 nM Nov 04 2019
S8550 AMG-176 AMG-176 is a selective MCL1 inhibitor with Ki values of 0.06 nM, 0.7 μM and 0.95 μM for MCL-1, Bcl-xL and Bcl-2 respectively. Nov 04 2019
S8586 Nedisertib (M3814, MSC2490484A) Nedisertib (M3814, MSC2490484A) is an orally bioavailable, highly potent and selective inhibitor of DNA activated protein kinase (DNA-PK) with an IC50 less than 3 nM. Nov 04 2019
S8784 PQR620 PQR620 is a novel, selective, orally bioavailable and brain penetrant dual TORC1/2 inhibitor. PQR620 has anti-tumor activity across 56 lymphoma models with a median IC50 of 250 nM after 72 h of exposure. Nov 04 2019
S8590 GSK 2837808A GSK2837808A is a selective LDHA (lactate dehydrogenase A) inhibitor with IC50 values of 1.9 nM and 14 nM for LDHA and LDHB respectively. Nov 04 2019
S8850 JH-RE-06 JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS). Nov 04 2019
S8875 MKC8866 MKC8866, a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29 μM for human IRE1α in vitro. Nov 04 2019
P1039 Somatostatin Acetate Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 1 nM. Nov 04 2019
S7765 Dovitinib (TKI258) Lactate Dovitinib (TKI258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4. Nov 01 2019
S7164 GSK343 GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces autophagy. Nov 01 2019
S8045 KU-0060648 KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM. Nov 01 2019
S1011 Afatinib (BIBW2992) Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy. Oct 31 2019
S2446 Levosimendan Levosimendan is a calcium sensitizer acting through calcium-dependent binding to cardiac troponin C (cTnC), provides treatment for heart failure. Oct 31 2019
S1228 Idarubicin HCl Idarubicin HCl is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Oct 31 2019
S7483 DMOG DMOG is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy. Oct 30 2019
Cat.No. Product Name Information Added
S1104 GDC-0879 GDC-0879 is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases. Oct 28 2019
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2. Oct 28 2019
S1110 Varespladib (LY315920) Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM. Phase 3. Oct 28 2019
S1113 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1. Oct 28 2019
S1409 Alfuzosin HCl Alfuzosin HCl is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH). Oct 28 2019
S1114 JNJ-38877605 JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. Phase 1. Oct 28 2019
S1115 Odanacatib (MK-0822) Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrated high selectivity versus off-target cathepsin B, L, S. Phase 3. Oct 28 2019
S1112 SGX-523 SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1. Oct 28 2019
S1084 Brivanib (BMS-540215) Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3. Oct 27 2019
S1034 NVP-AEW541 NVP-AEW541 is a potent inhibitor of IGF-1R/InsR with IC50 of 150 nM/140 nM in cell-free assays, greater potency and selectivity for IGF-1R in a cell-based assay. Oct 25 2019
S6552 CYM5541 CYM5541 is a selective, allosteric agonist of S1P3 with an EC50 of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes in vitro: S1P1 EC50 > 10 μM, S1P2 EC50 > 50 μM, S1P4 EC50 > 50 μM, and S1P5 EC50 > 25 μM. Oct 24 2019
S6724 SR1001 SR1001 is a RORα inverse agonist with Ki values of 172 nM and 111 nM for RORα and RORγ respectively. Oct 24 2019
S6734 PF-670462 PF-670462 is a potent and selective inhibitor of CK1ε and CK1δ with IC50 value of 90 nM and 13 nM, respectively. Oct 24 2019
S6618 JNJ-42153605 JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM. Oct 24 2019
S6620 Danirixin (GSK1325756) Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 binding = 12.5 nM), selective, and reversible CXCR2 antagonist. Oct 24 2019
S7791 Phorbol 12-myristate 13-acetate (PMA) Phorbol 12-myristate 13-acetate (PMA), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P). Oct 22 2019
S7775 Emricasan Emricasan is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection. Oct 22 2019
S2855 MRS 2578 MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors. Oct 22 2019
S4002 Sitagliptin phosphate monohydrate Sitagliptin phosphate monohydrate is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts. Oct 21 2019
S1322 Dexamethasone Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients. Oct 20 2019
Cat.No. Product Name Information Added
S6605 AR7 AR7 is a retinoic acid receptor α (RARα) antagonist. Oct 20 2019
S8479 LLY-284 LLY-284 is the diastereomer of LLY-283, which is a potent and selective SAM-competitive chemical probe for PRMT5. LLY-284 is much less active than LLY-283 and can be used as a negative control for LLY-283. Oct 20 2019
S1811 Amiloride HCl Amiloride is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM). Oct 18 2019
S3076 Foscarnet Sodium Foscarnet Sodium inhibits viral RNA polymerases, reverse transcriptase, and DNA polymerases through noncompetitive inhibition with dNTPs. Oct 17 2019
S7716 TAS-116 TAS-116 is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L). Oct 16 2019
S8792 UAMC-3203 UAMC-3203 is an improved ferroptosis inhibitor with an IC50 value of 10 nM in IMR-32 neuroblastoma cells. Oct 16 2019
S7076 T0901317 T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively. Oct 15 2019
S4673 Etonogestrel Etonogestrel is a synthetic form of the naturally occurring female sex hormone progesterone. It binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor mediated gene expression. Oct 15 2019
S9015 Homoharringtonine Homoharringtonine, a plant alkaloid with antitumor properties, inhibits protein translation by preventing the initial elongation step of protein synthesis via an interaction with the ribosomal A-site. Homoharringtonine reversiblely inhibits IL-6-induced STAT3 Tyrosine 705 phosphorylation and reduced anti-apoptotic proteins expression. Oct 14 2019
S4158 Ceftriaxone disodium salt hemi(heptahydrate) Ceftriaxone disodium salt hemi(heptahydrate) is a third-generation cephalosporin antibiotic. Oct 13 2019
S2842 SAR131675 SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc. Oct 12 2019
S1026 Imatinib Mesylate (STI571) Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy. Oct 11 2019
S5698 Ketorolac tromethamine salt Ketorolac tromethamine is a synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic and antipyretic properties. It is a non-selective COX inhibitor with IC50s of 20 nM for both COX-1 and COX-2. Oct 11 2019
S1646 Ketorolac Ketorolac is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively. Oct 11 2019
S6551 Adelmidrol Adelmidrol is an analogue of palmitoylethanolamide (PEA) with anti-inflammatory activities. Oct 10 2019
S8860 Cintirorgon (LYC-55716) Cintirorgon (LYC-55716) is a selective, first-in-class, oral, small-molecule investigational agent that selectively activates RORγ. Oct 10 2019
S6588 Methylprednisolone hemisuccinate Methylprednisolone sodium succinate is a glucocorticoid used to treat a variety health issues including severe allergic reactions, asthma, autoimmune diseases, blood disorders, gastrointestinal diseases and endocrine disorders. Oct 10 2019
S5644 Ceftriaxone Sodium Ceftriaxone Sodium is the sodium salt form of ceftriaxone, a beta-lactam, third-generation cephalosporin antibiotic with bactericidal activity. Oct 10 2019
S2799 Daporinad (FK866, APO866) Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2. Oct 10 2019
S8862 PDD00017273 PDD00017273 is a potent and selective poly (ADP ribose) glycohydrolase (PARG) inhibitor with an IC50 of 26 nM. PDD00017273 exhibits >350-fold selectivity for PARG over a panel of ion channels, enzymes and receptors, including PARP1 and ARH3. Oct 10 2019
Cat.No. Product Name Information Added
S2931 Aurora Kinase Inhibitor III Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase with an IC50 of 42 nM and has high selectivity for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively). Oct 10 2019
S6572 ML335 ML335 is a potent and selective TREK-1/2 activator. ML335 is an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively. Oct 10 2019
S8877 Imidazole ketone erastin Imidazole ketone erastin (IKE) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis. Oct 10 2019
A2009 Rituximab (anti-CD20) Rituximab (anti-CD20) is a chimeric anti-CD20 mAb that binds the CD20 antigen on B cells with a binding affinity of 5 nM, MW: 143.86 KD. Oct 10 2019
S8828 Gboxin Gboxin is an inhibitor of oxidative phosphorylation in cancer cells. It specifically inhibits the growth of primary mouse and human glioblastoma cells but not that of mouse embryonic fibroblasts or neonatal astrocytes. Oct 10 2019
S2043 Memantine HCl Memantine HCl is an antagonist of NMDAR. It is also a CYP2B6 and CYP2D6 inhibitor for recombinant CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively. Oct 09 2019
S7430 SB-3CT SB-3CT is an effective and selective gelatinase inhibitor with Ki of 13.9 nM and 600 nM for MMP-2 and MMP-9, respectively. Oct 09 2019
S2556 Rosiglitazone Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis. Oct 09 2019
S7665 CH5183284 (Debio-1347) CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1. Oct 09 2019
S7800 A-1155463 A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM). Oct 09 2019
S8358 WNK463 WNK463 is a pan-WNK-kinase inhibitor. It potently inhibits the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4). Oct 09 2019
S8245 Thiomyristoyl Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM. It inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM. Oct 08 2019
S2890 PF-562271 PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Oct 08 2019
S7885 SBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. Oct 07 2019
S5582 Cytarabine hydrochloride Cytarabine is a pyrimidine nucleoside analog that is used mainly in the treatment of leukemia. It is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. Sep 28 2019
S7071 (+)-Bicuculline (+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels. Sep 26 2019
S6499 PF-6260933 PF-6260933 is a potent inhibitor of MAP4K4 with an IC50 of 3.7 nM, possessing excellent kinome selectivity. Sep 25 2019
S8520 Senexin A Senexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively. Sep 24 2019
S7587 INCB024360 analogue INCB024360 analogue is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM. Sep 24 2019
S6192 N,N-Dimethylformamide(DMF) N,N-Dimethylformamide (DMF) is a polar organic solvent with a wide range of industrial applications. Sep 24 2019
Cat.No. Product Name Information Added
S7261 Beta-Lapachone Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2. Sep 24 2019
S6581 Fosamprenavir calcium salt Fosamprenavir is a pro-drug of the protease inhibitor and antiretroviral drug amprenavir. It is used for the treatment of HIV-1 infections. Sep 24 2019
S7455 Resatorvid (TAK-242) Resatorvid (TAK-242) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM. Resatorvid inhibits autophagy. Sep 24 2019
S1102 U0126-EtOH U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity. Sep 23 2019
S1082 Vismodegib (GDC-0449) Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay. Sep 20 2019
S5213 Piroctone Olamine Piroctone Olamine is a wide spectrum antibacterial and antifungal agent used in the treatment of dandruff,fungal infections. Sep 19 2019
S8832 Branebrutinib (BMS-986195) Branebrutinib (BMS-986195) is a potent inhibitor of BTK with IC50 values of 0.1 nM, 0.9 nM, 1.5 nM, 5 nM for BTK, TEC, BMX, TXK, respectively. Sep 17 2019
S6494 CCCP CCCP, an oxidative phosphorylation inhibitor, is a protonophore mitochondrial uncoupler that increases membrane permeability to protons, leading to a disruption in the mitochondrial membrane potential. Carbonyl cyanide 3-chlorophenylhydrazone (CCCP), the protonophore, can inhibits STING-mediated IFN-β production via disrupting mitochondrial membrane potential (MMP). Sep 17 2019
S6546 PD153035 PD153035 is a specific and potent inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (Ki = 5.2 pM). Sep 17 2019
S6531 Bohemine Bohemine is a CDK inhibitor with IC50s of 4.6, 83, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Sep 17 2019
S6530 EBE-A22 EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive. Sep 17 2019
S6602 TB5 TB5 is a potent and selective MAO-B inhibitor with Ki values of 110 and 1,450 nM for MAO-B and MAO-A, respectively. Sep 17 2019
S6568 ML346 ML346 is a Hsp70 activator and a novel modulator of proteostasis for protein conformational diseases. Sep 17 2019
S6564 ML348 ML348 is a potent and selective APT1 (Acyl protein thioesterase 1) inhibitor with Ki values of 280 nM and >10 μM for APT1 and APT2, respectively. Sep 17 2019
S6540 NG 52 NG-52 is a tri-substituted purine that binds to the ATP-binding site of yeast cyclin-dependent kinases, inhibiting Cdc28p and Pho85p with IC50s of 7 and 2 μM, respectively. Sep 17 2019
S6539 ASP5878 ASP5878 is a novel FGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively. Sep 17 2019
S6606 CDD3505 CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity. Sep 17 2019
S6607 YL-109 YL-109 is a novel antitumor agent that has ability to inhibit breast cancer cell growth and invasiveness in vitro and in vivo. Sep 17 2019
S6526 SKLB 610 SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR. Sep 17 2019
S6534 CZC-54252 CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for human wild type LRRK2 and G2019S LRRK2, respectively. Sep 17 2019
Cat.No. Product Name Information Added
S4421 Josamycin Josamycin is a macrolide antibiotic from Streptomyces narbonensis. The drug has antimicrobial activity against a wide spectrum of pathogens. Sep 17 2019
S6579 RCGD423 RCGD-423 is a modulator of gp130 signalling that regulates cartilage growth and differentiation. Sep 17 2019
S6560 PDM2 PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist. Sep 17 2019
S6589 Norethisterone Enanthate Norethisterone Enanthate is a form of progestogen-only injectable birth control which is used to prevent pregnancy in women. Sep 17 2019
S6583 Apraclonidine HCl Apraclonidine, also known as iopidine, is a sympathomimetic used in glaucoma therapy. It is an alpha2-adrenergic agonist. Sep 17 2019
S6582 Ozenoxacin Ozenoxacin is a quinolone antibiotic used for the treatment of impetigo. Sep 17 2019
S8809 MC180295 MC180295 is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs. Sep 17 2019
S6593 Methylprednisolone sodium succinate Methylprednisolone sodium succinate is a corticosteroid medication that reduces inflammation. Sep 17 2019
S8865 BAI1 BAI1 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM. Sep 17 2019
S6703 CMC-Na Sodium carboxymethyl cellulose (CMC-Na) is one of the important modified cellulose, a water-soluble cellulose, which is widely used in many application of food, pharmaceuticals, detergent, paper coating, dispersing agent, and others. Sep 17 2019
S6704 PEG300 PEG300 is a water-miscible polyether widely used in biochemistry, structural biology, and medicine in addition to pharmaceutical and chemical industries. It serves as a kind of solubilizer, excipient, lubricant, and chemical reagent. Sep 17 2019
S6705 PEG400 Polyethylene glycol 400 (PEG400) is a commonly used co-solvent used in a variety of pharmaceutical formulations. Sep 17 2019
S4599 Benzyl benzoate Benzyl benzoate is one of the older preparations used to treat scabies. Scabies is a skin infection caused by the mite sarcoptes scabiei. Sep 16 2019
P1085 Angiotensin II human Acetate Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 1 nM. Sep 15 2019
S3153 Levalbuterol tartrate Levalbuterol HCl is a relatively selective beta2-adrenergic receptor agonist used for the treatment of asthma. Sep 11 2019
S8867 Bentamapimod (AS602801) Bentamapimod (AS602801) is a novel, orally active JNK inhibitor with IC50 values of 80 nM, 90 nM and 230 nM for JNK1, JNK2 and JNK3 respectively. Sep 10 2019
S8859 BMS-1166 BMS-1166 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 interaction with an IC50 of 1.4 nM. Sep 10 2019
S2188 Phenprocoumon Phenprocoumon(Marcumar) is a vitamin K reductase with an IC50 of 1 μM Sep 09 2019
S8746 H3B-5942 H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values are 1 nM and 0.41 nM, respectively. Sep 06 2019
S6590 Hydrocortisone butyrate Hydrocortisone butyrate is a potent topical corticosteroid that can be used to treat a range of inflammatory skin conditions. Sep 06 2019
Cat.No. Product Name Information Added
S5797 Metyrosine Metyrosine, an antihypertensive drug, is a tyrosine hydroxylase inhibitor. Sep 06 2019
S8872 GSK8612 GSK8612 is a highly potent and selective inhibitor for TBK1 (Tank-binding Kinase-1) with pKd of 8.0. Within 10-fold affinity with respect to TBK1, no off-targets of GSK8612 could be identified. Sep 06 2019
S6592 Diquafosol Tetrasodium Diquafosol Tetrasodium, a P2Y2 receptor agonist, is a pharmaceutical drug for the treatment of dry eye disease. Sep 06 2019
S8871 Omadacycline tosylate Omadacycline is a first-in-class aminomethylcycline antibiotic, demonstrating antimicrobial activity in vitro against a range of Gram-positive and Gram-negative aerobes and some anaerobic bacteria. Sep 06 2019
S6587 Clobetasone butyrate Clobetasone butyrate is a new corticosteroid that is often employed topically as a treatment for a variety of conditions such as eczema, psoriasis, various forms of dermatitis, and also for certain ophthalmologic conditions. Sep 06 2019
S4622 3,4-Diaminopyridine 3,4-Diaminopyridine blocks presynaptic potassium channels, and subsequently prolongs the action potential and increases presynaptic calcium concentrations. It is a drug predominantly used in the treatment of a number of rare muscle diseases. Sep 06 2019
S8864 ZT-12-037-01 ZT-12-037-01 is a specific and ATP-competitive STK19 inhibitor with IC50s of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. It displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 μM. Sep 06 2019
S6585 Triethylenetetramine Dihydrochloride Triethylenetetramine, a Cu(II)-selective chelator, is commonly used for the treatment of Wilson's disease. Sep 06 2019
S7280 Edoxaban tosylate Monohydrate Edoxaban is a selective factor Xa inhibitor with Ki of 0.561 nM, >10 000-fold selectivity over thrombin and FIXa, and is also an orally bioavailable anticoagulant drug. Sep 05 2019
S5275 Testolone (RAD140) RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors. Sep 02 2019
S3019 Ciclopirox ethanolamine Ciclopirox ethanolamine (Ciclopirox olamine, HOE 296) is a broad-spectrum antifungal agent working as an iron chelator. Sep 02 2019
S1673 Aminophylline Aminophylline is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist. Sep 02 2019
S6197 Dimethylamine hydrochloride Dimethylamine is a precursor to several industrially significant compounds. Sep 02 2019
S6210 Ethanolamine hydrochloride Ethanolamine is a viscous, hygroscopic amino alcohol with an ammoniacal odor. It is widely distributed in biological tissue and is a component of lecithin. Sep 02 2019
S6232 Methylamine hydrochloride Methylamine is used as a building block for the synthesis of many other commercially available compounds. Sep 02 2019
S8699 SNS-314 Mesylate SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Sep 01 2019
S1154 SNS-314 SNS-314 is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1. Sep 01 2019
S8869 UNBS5162 UNBS5162 is a pan-antagonist of CXCL chemokine expression with in vitro cytotoxic activity (IC50 range of 0.5-5 µM) against a range of human cancer cell lines including glioblastoma (Hs683 and U373MG), colorectal (HCT-15 and LoVo), non-small-cell lung (A549) and breast (MCF-7). Aug 30 2019
S6612 Betazole Dihydrochloride Betazole Dihydrochloride is a histamine H2 agonist used clinically to test gastric secretory function. Aug 30 2019
S6576 BW-A78U BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity. Aug 30 2019
Cat.No. Product Name Information Added
S6577 PKC-theta inhibitor PKC-theta inhibitor (compound 20) inhibits PKC-θ with an IC50 of 18 nM. Aug 30 2019
S6578 Longdaysin Longdaysin is a Casein Kinase inhibitor with IC50 values of 8.8 μM, 5.6 μM, 52 μM and 29 μM for CKIδ, CKIα, ERK2 and CDK7. Aug 30 2019
S6569 VUF10460 VUF10460 is a histamine H4 receptor agonist. Aug 30 2019
S6611 Cyclothiazide Cyclothiazide is a positive allosteric modulator of ionotropic α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA)-type glutamate receptors with critical roles in neurological development and function. Aug 30 2019
S6613 Vanillylmandelic acid Vanillylmandelic acid (VMA) is a chemical intermediate in the synthesis of artificial vanilla flavorings and is an end-stage metabolite of the catecholamines Aug 30 2019
S6557 ML355 ML355 is a potent and selective inhibitor of human 12-Lipoxygenase with an IC50 of 290 nM and shows excellent selectivity over related lipoxygenases and cyclooxygenases. Aug 30 2019
S6550 URB602 URB602 is an inhibitor of monoacylglycerol lipase (MGL), a serine hydrolase involved in the biological deactivation of the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG). Aug 30 2019
S6549 PBTZ169 PBTZ169, an antibiotic with antimycobacterial activity, is an irreversible inhibitor of DprE1. Aug 30 2019
S6580 D-Luciferin Potassium Salt D-Luciferin is a substrate for the enzyme firefly luciferase. Aug 30 2019
S6571 BQR695 BQR695 is a quinoxaline that displays sub-micromolar potency against human PI4KIIIβ (IC50~90 nM). Aug 30 2019
S6574 KDU691 KDU691 is a Plasmodium PI4K-specific inhibitor with IC50 values of 0.18 μM and 0.061 μM against hypnozoite forms and liver schizontsm, respectively. Aug 30 2019
S6573 MD2-IN-1 MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD value of 189 μM. Aug 30 2019
S6566 NSC23005 Sodium NSC 23005 is a small molecule inhibitor of p18 (ED50=5.21 nM). Aug 30 2019
S6554 ML365 ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3). Aug 30 2019
S6555 AZD2098 AZD2098 is a potent and bioavailable CCR4 receptor antagonist with pIC50 of 7.8. Aug 30 2019
S6567 Src Inhibitor 1 Src Inhibitor 1 is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes. Aug 30 2019
S6562 KKL-35 KKL-35 inhibits the trans-translation tagging reaction with an IC50 of 0.9 µM. It has broad-spectrum antibiotic activity. Aug 30 2019
S6565 JK184 JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells. Aug 30 2019
S6561 4-IBP 4-IBP is a selective σ1 receptor agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 nM). Aug 30 2019
S6614 Fursultiamine Fursultiamine is a nutritional supplement and vitamin B1 derivative, with potential antineoplastic activity. Aug 30 2019
Cat.No. Product Name Information Added
S8162 Upadacitinib (ABT-494) Upadacitinib (ABT-494) is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1. Aug 30 2019
S7801 A-1331852 A-1331852 is a potent and selectiveBCL-XL inhibitor with Ki value less than 0.01 nM for BCL-XL and 6 nM, 4 nM, 142 nM for Bcl-2, Bcl-W, MCL-1 respectively. It may be useful in the treatment of cancer, immune and autoimmune diseases. Aug 29 2019
A2013 Durvalumab (anti-PD-L1) Durvalumab (anti-PD-L1) is a selective, high affinity human IgG1 mAb that blocks programmed cell death ligand-1 (PD-L1) binding to PD-1 (IC50=0.1 nM) and CD80 (IC50=0.04 nM). MW=146.3 kDa. Aug 28 2019
A2006 Bevacizumab (anti-VEGF) Bevacizumab (anti-VEGF) is a humanized anti-VEGF monoclonal antibody which binds to and neutralizes all human VEGF-A isoforms and bioactive proteolytic fragments, MW:149 KD. Aug 28 2019
A2007 Trastuzumab (anti-HER2) Trastuzumab (anti-human HER2) is a humanized, recombinant monoclonal antibody that binds to the extracellular domain of HER2, MW:145.53 KD. Aug 28 2019
A2008 Pertuzumab (anti-HER2) Pertuzumab (anti-HER2), a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD. Aug 28 2019
A2010 Adalimumab (anti-TNF-alpha) Adalimumab (anti-TNF-alpha) is the first fully human, recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha, MW: 144.19 KD. Aug 28 2019
A2011 Sarilumab (anti-IL-6Rα) Sarilumab (anti-IL-6Rα) is a fully human anti-IL-6Rα mAb that binds membrane-bound and soluble human IL-6Rα with high affinity, MW: 144.13 KD. Aug 28 2019
A2012 Tocilizumab (anti-IL-6R) Tocilizumab (anti-IL-6R) is a humanized monoclonal antibody that binds to the interleukin-6 receptor, MW: 148 KD. Aug 28 2019
A2000 Cetuximab (anti-EGFR) Cetuximab, a novel molecular-targeted agent,is an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR to block ligand stimulation. MW:145.781 KD. Aug 28 2019
A2001 Ipilimumab (anti-CTLA-4) Ipilimumab (anti-CTLA-4) is an immunomodulatory monoclonal antibody directed against the cell surface antigen CTLA-4 and also a type of immune checkpoint inhibitor. MW : 148 kD. Aug 28 2019
A2002 Nivolumab (anti-PD-1) Nivolumab (anti-PD-1) is a genetically engineered, fully human immunoglobulin (Ig) G4 monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed death-1 (PD-1,PCD-1) with immune checkpoint inhibitory and antineoplastic activities. MW : 143.597 KD. Aug 28 2019
A2004 Atezolizumab (anti-PD-L1) Atezolizumab (anti-PD-L1) is a fully humanized, IgG1 monoclonal antibody that blocks the interaction of PD-L1 with both PD-1 and B7.1, but not the interaction of PD-L2 with PD-1. MW : 145 KD. Aug 28 2019
A2016 Camrelizumab (anti-PD-1) Camrelizumab (anti-PD-1) is a humanized anti-PD-1 IgG4 antibody that blocks the binding of PD-L1 and PD-L2 to PD-1 with immune checkpoint inhibitory and antineoplastic activities. Aug 28 2019
A2017 Spartalizumab (anti-PD-1) Spartalizumab (anti-PD-1) is a humanized anti-PD-1 IgG4 antibody that blocks the binding of PD-L1 and PD-L2 to PD-1. It binds to PD-1 with high affinity and inhibits the biological activity of PD-1. Aug 28 2019
S9028 Cimifugin Cimifugin is a bioactive component of Saposhnikovia divaricata, a Chinese herb for treating allergy. Aug 26 2019
S5815 WAY-316606 WAY-316606, a specific antagonist of SFRP1, functions as an activator of canonical Wnt/β-catenin signalling in the human hair bulb. Aug 26 2019
S6414 Apilimod Apilimod is a cell permeable small molecule that specifically inhibits PIKfyve with an IC50 of 14 nM in an in vitro kinase assay. It is also an inhibitor of IL-12/23 and shows no activity toward other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K isoforms. Aug 26 2019
S8495 WT161 WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. Aug 26 2019
S1219 YM201636 YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). Aug 26 2019
Cat.No. Product Name Information Added
S1489 PIK-93 PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; shown to inhibit PI3Kα with IC50 of 39 nM. Aug 26 2019
S5234 Nintedanib Ethanesulfonate Salt Nintedanib is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively. Aug 25 2019
S6522 ST 271 ST271 is a tyrphostin-like protein tyrosine kinase (PTK) inhibitor which inhibits phospholipase D (PLD) activity. Aug 20 2019
S6525 AG 555 AG-555 is an inhibitor of tyrosine kinase, interacts directly with topoisomerase I, thus preventing DNA relaxation. It inhibits EGFR with an IC50 of 0.7 μM. Aug 20 2019
S6535 SU1498 SU1498, a powerful inhibitor of KDR (IC50 = 0.7 μM), stimulates accumulation of phosphorylated ERK1/2 in endothelial cells. Aug 20 2019
S6509 AG 494 AG-494, a member of the tyrphostin family of tyrosine kinase inhibitors, is a potent inhibitor of EGF receptor autophosphorylation (IC50=1.2 μM) and EGF-dependent cell growth (IC50=6 μM). Aug 20 2019
S6523 RG14620 RG14620, an EGFR inhibitor of the tyrphostin family, directly inhibits the transport function of ABCG2. Aug 20 2019
S6492 Doravirine (MK-1439) Doravirine is a novel HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50 values of 12, 9.7, and 9.7 nM against the wild type (WT) and K103N and Y181C reverse transcriptase (RT) mutants, respectively, in a biochemical assay. It is highly specific with minimum off-target activities. Aug 20 2019
S6532 kb-NB77-78 kb-NB77-78 is an analog of CID797718. However, it shows no inhibitory activty towards PKD1. Aug 16 2019
S5374 5'-Cytidylic acid 5'-Cytidylic acid is a nucleotide that is used as a monomer in RNA. Aug 15 2019
S6529 NIH-12848 NIH-12848 is a specific PI5P4Kγ inhibitor with an IC50 of approximately 1 μM but does not inhibit the α and β PI5P4K isoforms at concentrations up to 100 μM. Aug 13 2019
S6537 CVT-313 CVT-313 is a potent CDK2 inhibitor with an IC50 of 0.5 microM in vitro. It has no effect on other, nonrelated ATP-dependent serine/threonine kinases. Aug 13 2019
S6511 RIPA-56 RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor. Aug 13 2019
S8735 BI-3812 BI-3812 is a highly potent and efficacious BCL6 inhibitor probe compound with an IC50 less than 3 nM. Aug 13 2019
S6496 Genz-123346 free base Genz-123346 is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1, the first step in the biosynthesis of gangliosides and other glycosphingolipids. Aug 13 2019
S6502 SD 0006 SD0006 is an inhibitor of p38 kinase-alpha (p38alpha) with IC50 values of 0.016 μM and 0.677 μM for p38α and p38β. It is selective for p38α kinase over 50 other kinases screened (including p38γ and p38δ with modest selectivity over p38β). Aug 13 2019
S6510 Iso-H7 dihydrochloride Iso-H7 dihydrochloride is an inhibitor of phosphokinase C. Aug 13 2019
S6495 6-Bromo-2-hydroxy-3-methoxybenzaldehyde 6-Bromo-2-hydroxy-3-methoxybenzaldehyde is a bromobenzaldehyde derivative that participates in the synthesis of (±)-norannuradhapurine.6-Bromo-2-hydroxy-3-methoxybenzaldehyde is an IRE-1α inhibitor with an IC50 of 0.08 μM. Aug 13 2019
S6504 BX517 BX517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket of the protein (IC50 = 6 nM). Aug 13 2019
S6508 Mitapivat Mitapivat is an activator of a pyruvate kinase PKM2, an enzyme involved in glycolysis. Aug 13 2019
Cat.No. Product Name Information Added
S5415 Enoxaparin sodium Enoxaparin sodium is a low-molecular-weight heparin used to prevent and treat deep vein thrombosis or pulmonary embolism. It binds to and accelerates the activity of antithrombin III. Aug 13 2019
S6503 LX2343 LX2343 is a multi-target agent that exhibits a high capability for ameliorating multi-abnormalities of AD pathogenesis. It is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. Aug 13 2019
S6506 Compound 401 Compound 401 is a synthetic inhibitor of DNA-PK and mTOR (IC50=5.3 μM). It has no inhibition on p110α/p85α PI3K (>100 μM) and blocks the phosphorylation of S6 kinase 1 Thr389 and Akt Ser473 in COS7 cells. Aug 13 2019
S6512 Defensamide (MHP) Defensamide (MHP) is an activator of sphingosine kinase (SPHK1). It can modulate the innate epidermal immune response by potentiating SPHK1 activity and inducing cAMP production. Aug 13 2019
S6497 SMI-16a SMI-16a is a selective Pim kinase inhibitor with IC50 values of 150 nM and 20 nM for Pim1 and Pim2 respectively. Aug 13 2019
S6498 T56-LIMKi T56-LIMKi is a selective inhibitor of LIMK2. Aug 13 2019
S8826 BAY-293 BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM. Aug 13 2019
S7324 TMP269 TMP269 is a potent, selective class IIa HDAC inhibitor with IC50 of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively. Aug 13 2019
S8568 G1T38 Lerociclib (G1T38) is a novel, potent, selective, and orally bioavailable CDK4/6 inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively. Aug 13 2019
S6500 KX1-004 KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM). Aug 13 2019
S8787 GSK'547 GSK'547 is a highly selective and potent inhibitor of RIP1 (RIPK1) exhibiting a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963 Aug 13 2019
S6533 Briciclib Briciclib is a water soluble derivative of ON-013100, a small molecule that binds to and inhibits eukaryotic translation initiation factor 4E (eIF4E). Aug 13 2019
S6507 KN-92 phosphate KN-92 is an inactive derivative of KN-93, the selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII). Aug 13 2019
S8842 BAY-218 BAY-218 is a potent and selective small-molecule AhR inhibitor, inhibiting AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands. Aug 13 2019
S6545 BI-4464 BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. Aug 13 2019
S6524 NSC 42834 NSC42834 is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2 with IC50 values between 10 and 30 μM. Aug 13 2019
S6541 MTX-211 MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase. Aug 13 2019
S8484 GSK2982772 GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase (RIPK1) inhibitor with the IC50 value of 16 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses. Aug 13 2019
S8642 GSK'963 GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase (RIPK1) with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases. Aug 13 2019
S6608 AL082D06 AL082D06 is a nonsteroidal glucocorticoid receptor (GR) antagonist with no detectable binding affinity for the highly related receptors for mineralocorticoids, androgens, estrogens, and progestins. Aug 13 2019
Cat.No. Product Name Information Added
S6609 JZL195 JZL195 is a potent inhibitor of both FAAH and MAGL with IC50s of 2 and 4 nM respectively. Aug 13 2019
S6610 GSK2981278 GSK2981278 is a highly potent and selective inverse agonist for RORγ. Aug 13 2019
S6538 B-Raf IN 1 B-Raf IN 1 is an inhibitor of Raf wih IC50 values of 24 nM and 25 nM for B-Raf and C-Raf respectively. It is selective over 13 other kinases, including PKCα, IKKβ, and PI3Kα. Aug 13 2019
S6527 Kobe2602 Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM). Aug 13 2019
S6518 Desmethylanethol trithione Desmethylanethol trithione (ADT-OH) is a derivative of anethole dithiolethione (ADT) and synthetic hydrogen sulfide (H2S) donor. Aug 13 2019
S6536 TTP 22 TTP22 is a casein kinase 2 (CK2) inhibitor with an IC50 value of 100 nM. It displays selectivity for CK2 over JNK3, ROCK1, and MET with no inhibitory effects towards these kinases at 10 μM. Aug 13 2019
S8854 JNJ-38877618(OMO-1) JNJ-38877618 (OMO-1) is a potent, highly selective, orally bioavailable MET kinase inhibitor with binding affinity (Kd) of 1.4 nM and enzyme inhibitory activity against wt and M1268T mutant MET (2 and 3 nM IC50). Aug 13 2019
S8297 ARV-825 ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC. Aug 13 2019
S8722 ICEC0942 (CT7001) ICEC0942 (CT7001) is a new, orally bioavailable CDK7 inhibitor with an IC50 of 40nM. The IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. Aug 13 2019
S8676 Glumetinib (SCC244) Glumetinib (SCC244) is a potent and highly selective c-Met inhibitor with an IC50 of 0.42 ± 0.02 nmol/L. Glumetinib has greater than 2,400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, and TyrO3. Aug 13 2019
S8169 GSK481 GSK481 is a RIP1(Receptor Interacting Protein Kinase1, RIPK1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death. Aug 13 2019
S5266 Stiripentol Stiripentol is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450. Aug 08 2019
S8287 CPI-455 HCl CPI-455 is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents. Aug 08 2019
S8541 FM-381 FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively. Aug 08 2019
S3692 N-Ethylmaleimide (NEM) N-Ethylmaleimide (NEM) is an organic compound that is derived from maleic acid. It is an irreversible inhibitor of all cysteine peptidases, with alkylation occurring at the active site thiol group. Aug 07 2019
S9321 Topotecan Topotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases. Aug 07 2019
S2667 Dolutegravir (GSK1349572) Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. Aug 07 2019
S7663 Ruboxistaurin HCl(LY333531 ) LY333531 is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively. Aug 05 2019
S2057 Cyclophosphamide Monohydrate Cyclophosphamide Monohydrate is a nitrogen mustard alkylating agent, it attaches the alkyl group to the guanine base of DNA, shown to crosslink DNA, causing strand breakage and inducing mutations. Aug 02 2019
S1359 Losartan Potassium (DuP 753) Losartan is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM. Aug 01 2019
Cat.No. Product Name Information Added
S1415 Clopidogrel Bisulfate Clopidogrel is an oral, thienopyridine class antiplatelet agent. Aug 01 2019
S7370 4E1RCat 4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction, and inhibits the binding of eIF4G to eIF4E with IC50 of 3.2 μM. Jul 29 2019
S7369 4EGI-1 4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 μM. Jul 29 2019
S6521 WHI-P258 WHI-P258 is an inhibitor of JAK3 with Ki value of 72 μM. Jul 28 2019
S6519 R112 R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor with Ki value of 96 nM. Jul 28 2019
S6520 WHI-P180 WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET and kinase insert domain receptor (KDR), respectively. Jul 28 2019
S6513 HG-14-10-04 HG-14-10-04 is an inhibitor of ALK. Jul 28 2019
S6501 NVP 231 NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 12 nM. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage. Jul 28 2019
S6543 ZD-4190 ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively. Jul 28 2019
S6544 SR-3029 SR-3029 is a potent and selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 values of 44 and 260 nM for CK1δ and CK1ε, respectively. Jul 28 2019
S8643 AZD5991 AZD5991 is a macrocyclic MCL-1 inhibitor with sub-nanomolar affinity for MCL-1 (Ki = 0.13 nM). The binding affinity of AZD5991 is about 25-fold lower for mouse Mcl-1 vs. human Mcl-1 but only four-fold lower for rat Mcl-1. Jul 28 2019
S6505 X-376 X-376 is an ALK inhibitor and potentially useful in non-small cell lung cancer. Jul 28 2019
S6489 Lasmiditan succinate Lasmiditan succinate is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (Ki=2.21 nM) without vasoconstrictor activity. Jul 28 2019
S6490 Vadadustat Vadadustat is a novel, titratable, oral HIF-PH inhibitor. Jul 28 2019
S8830 AMG510 AMG-510 is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound. Jul 28 2019
S6412 Altiratinib Altiratinib is a potent single-digit nanomolar inhibitor of TRK, MET, TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits MET and MET mutant with IC50 values in the range of 0.3-6 nM. Jul 28 2019
S6516 GNE-477 GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR. Jul 28 2019
S2760 Canagliflozin Canagliflozin is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM in a cell-free assay, exhibits 413-fold selectivity over hSGLT1. Jul 25 2019
S4636 Teneligliptin hydrobromide Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM. Jul 25 2019
S7400 ISRIB (trans-isomer) ISRIB (trans-isomer), the trans-isomer of ISRIB, is a potent and selective PERK inhibitor with IC50 of 5 nM and does not have global effects on translation, transcription, or mRNA stability in non-stressed cells. Jul 23 2019
Cat.No. Product Name Information Added
S2248 Silmitasertib (CX-4945) Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2. Jul 22 2019
S1292 Chelerythrine Chloride Chelerythrine is a potent, selective antagonist of PKC with IC50 of 0.66 μM. Jul 21 2019
S5002 Fingolimod (FTY720) HCl Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells. Jul 19 2019
S8818 V-9302 V-9302 is a competitive small molecule antagonist of transmembrane glutamine flux, that selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) with an IC50 value of 9.6 μM for inhibition of glutamine uptake in HEK-293 cells. Jul 18 2019
S8600 Elenbecestat Elenbecestat is a novel BACE1 inhibitor, demonstrating prolonged reductions in plasma beta-amyloid levels after single dosing. Jul 18 2019
S5645 Hemin Hemin is an iron-containing porphyrin used in the management of porphyria attacks, particularly in acute intermittent porphyria.Hemin is an Heme oxygenase (HO)-1 inducer. Jul 17 2019
S7536 Lorlatinib (PF-6463922) PF-06463922 is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. PF-06463922 induces apoptosis. Phase 1. Jul 17 2019
S1271 Acarbose Acarbose is an inhibitor of intestinal alpha-glucosidase, used to treat type 2 diabetes mellitus. Jul 16 2019
S1698 Torsemide Torsemide is a pyridyl sulfonylurea with a chemical structure between that of traditional loop diuretics and Cl- channel blockers, used to treat hypertension. Jul 16 2019
S2610 Lonidamine Lonidamine is an orally administered small molecule hexokinase inactivator. Jul 16 2019
S7209 GSK650394 GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively. Jul 16 2019
S8077 RI-1 RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM. Jul 16 2019
S8368 LM10 LM10 is a selective tryptophan 2,3-dioxygenase (TDO) inhibitor with IC50 values of 0.62 and 2 μM for human and mouse TDO, respectively. Jul 16 2019
S8234 RS-1 RS-1 is a RAD51-stimulatory compound, which increases the DNA binding activity of RAD51. It is an HDR(homology-directed repair) enhancer that enhances Cas9- and TALEN-mediated knock-in efficiency in rabbit embryos both in vitro and in vivo. Jul 16 2019
S7447 ZLN005 ZLN005 is a potent and tissue-specific PGC-1α transcriptional activator. Jul 16 2019
S1858 Dienestrol Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist. Jul 16 2019
S2155 LY2608204 LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2. Jul 16 2019
S4701 2-Deoxy-D-glucose 2-Deoxy-D-glucose, an analog of glucose, is a glycolytic inhibitor with antiviral activity. 2-Deoxy-D-glucose induces apoptosis and inhibits Herpes Simplex Virus type-1 (HSV-1) receptor expression. Jul 16 2019
S2035 Epalrestat Epalrestat is an aldose reductase inhibitor with IC50 of 72 nM. Jul 16 2019
S3003 Prostaglandin E2 (PGE2) Prostaglandin E2 palys important effects in labour (softens cervix and causes uterine contraction) and also stimulates osteoblasts to release factors that stimulate bone resorption by osteoclasts. Jul 15 2019
Cat.No. Product Name Information Added
S4851 Tafluprost Tafluprost is a novel prostaglandin analog with a high affinity for the fluoroprostaglandin (FP) receptor PGF2α. A prostanoid selective FP receptor agonist. Jul 15 2019
S1508 Alprostadil Alprostadil is used as a drug in the treatment of erectile dysfunction and has vasodilatory properties. It is a Prostaglandin Analog and Prostaglandin E1 Agonist. Jul 15 2019
S7211 PF-04418948 PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1. Jul 15 2019
S7343 URMC-099 URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. Jul 15 2019
S4152 Ethamsylate Ethamsylate is a haemostatic drug, which inhibits biosynthesis and action of prostaglandins, and increases capillary endothelial resistance as and platelet adhesion. Jul 15 2019
S9327 Carboprost Carboprost is a synthetic prostaglandin analogue of PGF2α with oxytocic properties. Jul 15 2019
S8612 α-cyano-4-hydroxycinnamic acid(α-CHCA) 4-Chloro-α-cyanocinnamic acid (α-CHCA) is a classic monocarboxylate transporters (MCT) inhibitor. α-cyano-4-hydroxycinnamate (CHC) has a 10-fold selectivity for MCT1 compared to other MCTs. Jul 15 2019
S1407 Bimatoprost Bimatoprost is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension. Jul 15 2019
S5819 MRE-269(ACT-333679) MRE-269(ACT-333679) is a prostaglandin I2 (IP) receptor agonist with a binding affinity for the human IP receptor that is 130-fold greater than that for other human prostanoid receptor. Jul 15 2019
S4194 Azaguanine-8 Azaguanine-8 is a purine analogs showing antineoplastic activity by competing with guanine in the metabolism. Jul 15 2019
S4803 Thymidine Thymidine is a pyrimidine nucleoside that is composed of the pyrimidine base thymine attached to the sugar deoxyribose. As a constituent of DNA, thymidine pairs with adenine in the DNA double helix. Jul 15 2019
S3738 Travoprost Travoprost is a PGF2a analog that was launched as an ophthalmic solution administered topically for the treatment of elevated intraocular hypertension as a result of open-angle glaucoma, a common optic neuropathy, and a leading cause of blindness. It can act as an agonist of prostaglandin F receptor. Jul 15 2019
S5056 Dinoprost tromethamine Dinoprost Tromethamine is a synthetic analogue of the naturally occurring prostaglandin F2 alpha, which stimulates myometrial activity, relaxes the cervix, inhibits corpus luteal steroidogenesis, and induces luteolysis by direct action on the corpus luteum. Jul 15 2019
S8747 BAY-8002 BAY-8002 is a novel MCT1 inhibitor and potently suppress bidirectional lactate transport. BAY-8002 significantly increases intratumor lactate levels and transiently modulates pyruvate levels. Jul 15 2019
S8251 Necrosulfonamide Necrosulfonamide is a very specific and potent necrosis inhibitor and blocks mixed lineage kinase domain-like protein (MLKL). Jul 15 2019
S5749 Chlorpromazine Chlorpromazine is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Jul 15 2019
S2749 BGT226 maleate (NVP-BGT226 maleate) BGT226 (NVP-BGT226) is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2. Jul 14 2019
S8788 CH7057288 CH7057288 is a potent and selective TRK inhibitor with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB, and TRKC respectively. Jul 12 2019
S8743 SKLB-23bb SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability. Jul 12 2019
S6423 Tildipirosin Tildipirosin is a 16-membered ring, tribasic and semi-synthetic macrolide antibiotic. Jul 12 2019
Cat.No. Product Name Information Added
S8791 Zanubrutinib (BGB-3111) Zanubrutinib (BGB-3111) is a potent, specific and irreversible BTK inhibitor that has been shown to have a lower off-target inhibitory activity on other kinases, including ITK, JAK3 and EGFR. Jul 12 2019
S6427 AZ876 AZ876 is a novel high-affinity Liver X Receptor (LXR) agonist with Ki values of 0.007 μM and 0.011 μM for human LXRα and LXRβ respectively. Jul 12 2019
S6413 fexaramine Fexaramine is a potent, selective farnesoid X receptor (FXR) agonist with an EC50 of 25 nM and it displays no activity at hRXRα, hPPARα, hPPARγ, hPPARδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ and hVDR receptors. Jul 12 2019
S8795 FDL169 FDL169 is a CFTR corrector that is designed to fix and restore the function of the defective CFTR protein. Jul 12 2019
S6429 Coniferyl alcohol Coniferyl alcohol is an intermediate in biosynthesis of eugenol and of stilbene and coumarin. Jul 12 2019
S8821 GSK3179106 GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo. Jul 12 2019
S8793 ULK-101 ULK-101 is a potent and selective ULK1 inhibitor with IC50 values of 8.3 nM and 30 nM for ULK1 and ULK2, respectively. Jul 12 2019
S6459 Nifurtimox Nifurtimox is an antiprotozoal agent. Jul 12 2019
S6471 Lucanthone Lucanthone is a novel autophagic inhibitor and also an orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1. Jul 12 2019
S8823 ABX-1431 ABX-1431 is a highly potent, selective, and CNS-penetrant Monoacylglycerol lipase (MGLL) inhibitor with IC50 values of 14 nM and 27 nM for hMGLL and mMGLL respectively. Jul 12 2019
S8817 HS-10296 HS-10296 (Almonertinib, Ameile) is a small molecule inhibitor of EGFR-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR. Jul 12 2019
S8693 Selective PI3Kδ Inhibitor 1 (compound 7n) Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM]. Jul 12 2019
S8769 Tinostamustine(EDO-S101) Tinostamustine(EDO-S101) is a first-in-class alkylating deacetylase inhibitor with IC50 values of 9 nM, 9 nM, 25 nM and 107 nM for HDAC1, HDAC2, HDAC3 and HDAC8 (Class 1 HDACs) respectively and 6 nM, 72 nM for HDAC6 and HDAC10 (Class II HDACs). Jul 12 2019
S8846 compound 3i (666-15) Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells. Jul 12 2019
S5952 Baloxavir marboxil Baloxavir marboxil, a cap-endonuclease inhibitor, is an antiviral drug. Jul 12 2019
S8530 BAY 1436032 BAY-1436032 is a highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). It is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displays potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants. Jul 12 2019
S6484 uridine triacetate Uridine triacetate is an orally active prodrug of the naturally occurring nucleoside uridine. It is used for the treatment of hereditary orotic aciduria (Xuriden), or for the emergency treatment of fluorouracil or capecitabine overdose or toxicity. Jul 12 2019
S6488 Gadoxetate sodium Gadoxetate is a paramagnetic gadolinium-containing contrast agent in which its salt form, gadoxetate disodium, is used for intravenous injection. Jul 12 2019
S8704 iCRT14 iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay. Jul 12 2019
S6487 fluticasone furoate Fluticasone furoate is an inhaled corticosteroid/long-acting beta-agonist combination with a prolonged bronchodilator duration of action. It is used for the treatment of non-allergic and allergic rhinitis administered by a nasal spray. Jul 12 2019
Cat.No. Product Name Information Added
S8438 T-3775440 HCl T-3775440 HCl is an irreversible LSD1 inhibitor that is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nmol/L. Jul 12 2019
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