New Products

PI3K/Akt/mTOR
Catalog No. Product Name Information Added
S8779 Parsaclisib (INCB050465) Hydrochloride Parsaclisib (INCB050465, IBI376) Hydrochloride is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases. Jul 23 2021
S4460 IMM-H007 IMM-H007, an adenosine derivative, is an activator of AMP-Activated Protein Kinase (AMPK). IMM-H007 is a potential drug for treating cardiac dysfunction. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 (ATP binding cassette subfamily a member 1) degradation and facilitates its cell-surface localization in macrophages, thereby promotes cholesterol efflux. Jun 01 2021
S9860 BC1618 BC1618 is an orally active Fbxo48 inhibitor that stimulates adenosine monophosphate (AMP)-activated protein kinase (Ampk)-dependent signaling. BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity. May 24 2021
S9864 Elimusertib (BAY-1895344) Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM. Apr 27 2021
S5978 Gallein Gallein (Pyrogallol phthalein) is an inhibitor of G protein βγ (G beta-gamma complex, Gβγ) subunit interaction with PI3 kinase. Gallein inhibits β-ionone effects and exhibits anti-tumor activity. Gallein can be used as a biological stain. Apr 27 2021
S9638 BRD0705 BRD0705 is a potent, paralog selective and orally active inhibitor of GSK3α (Glycogen synthase kinase 3α) with IC50 of 66 nM and Kd of 4.8 μM. BRD0705 also inhibits GSK3β with IC50 of 515 nM. BRD0705 can be used for acute myeloid leukemia (AML). Apr 21 2021
S4572 Homosalate Homosalate (HMS, Homomenthyl salicylate) is an organic ultraviolet filter used in most sunscreens but has been reported to be toxic to marine organisms. Homosalate aggravates the invasion of human trophoblast cells as well as regulates intracellular signaling pathways including PI3K/AKT and MAPK pathways. Mar 30 2021
S7586 PS-48 PS-48 is an allosteric activator of phosphoinositide-dependent protein kinase-1 (PDK1). Mar 30 2021
S8917 ME-401 ME-401(PWT-143) is a potent and selective inhibitor of P110δ with IC50 of 8.4 nM. Feb 02 2021
S0041 UCB9608 UCB9608 (compound 44) is a potent, selective and orally bioavailable inhibitor of PI4KIIIβ with IC50 of 11 nM. UCB9608 is a potent immunosuppressive agent that improves metabolic stability and exhibits excellent pharmacokinetic profile. Dec 15 2020
JAK/STAT
Catalog No. Product Name Information Added
S0981 BD750 BD750 is an immunosuppressant and a dual inhibitor of JAK3 and STAT5 that inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation with IC50 of 1.5 μM and 1.1 μM for mouse and human T-cell proliferation, respectively. Feb 02 2021
S0374 GDC046 GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively. Jan 18 2021
S0384 RO495 RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2). Dec 29 2020
S0918 Ginkgolic acid C17:1 Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells. Nov 27 2020
S9664 Colivelin Colivelin (CLN) is a brain-penetrant neuroprotective peptide with potent long-term capacity against deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin is an activator of STAT3. Nov 27 2020
S0818 STAT3-IN-1 STAT3-IN-1 (compound 7d) is an excellent, selective and orally active inhibitor of STAT3 with IC50 of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 induces apoptosis of tumor cells. Sep 25 2020
S9676 PF-06826647 PF-06826647 (Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO). Sep 11 2020
S0437 SAR-20347 SAR-20347 is a potent inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50 of 0.6 nM, 23 nM, 26 nM and 41 nM, respectively. SAR-20347 inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling. Sep 02 2020
S0391 TG-89 TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM. May 26 2020
S1050 TCS PIM-1 1 TCS PIM-1 1 (SC 204330) 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
Cell Cycle
Catalog No. Product Name Information Added
S6000 CID44216842 CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor with EC50s of 1.0 μM and 1.2 μM for Cdc42WT and Cdc42Q61L mutant in GTP binding assay, respectively. Jul 29 2021
S6390 Y-27632 Y-27632 is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK. Jul 23 2021
S6884 LY3405105 LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity. Jul 16 2021
S6875 CASIN CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM. Jul 06 2021
S8911 BOS172722 BOS-172722 is a monopolar spindle 1 (MPS1) checkpoint inhibitor with IC50 of 2 nM. Jul 06 2021
S9859 BSJ-4-116 BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects. Jun 21 2021
S9880 MS140 MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC). Jun 21 2021
S3406 LDN-192960 LDN-192960 (Compd 1) is a potent inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50 of 10 nM and 48 nM, respectively. Jun 01 2021
S6214 H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively. May 31 2021
S9871 BTYNB BTYNB (BTYNB IMP1 Inhibitor, MDK6620) is a potent and selective inhibitor of IMP1 binding to c-Myc mRNA. BTYNB downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). BTYNB disrupts this enhancer function by impairing IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA association. May 24 2021
DNA Damage
Catalog No. Product Name Information Added
S9775 SCR130 SCR130 is a novel DNA repair inhibitor with IC50s of 14 μM in Reh cells and 2 μM in Nalm6 cells. SCR130 specifically inhibits DNA Ligase IV‐mediated joining with minimal or no effect on Ligase III and Ligase I mediated joining. Jul 26 2021
S3397 FEN1-IN-4 FEN1-IN-4 (FEN1 Inhibitor C2, JUN93587, Compound 2) is an inhibitor of human flap endonuclease-1 (hFEN1) with IC50 of 30 nM for hFEN1-336Δ. Jun 22 2021
S3549 PFM01 PFM01, a cell-permeable N-alkylated Mirin derivative, is a selective inhibitor of MRE11 endonuclease activity. Jun 08 2021
S0858 EG1 EG1 is a specific Paired box 2 (Pax2) inhibitor that targets the DNA binding domain and inhibits embryonic kidney development. Jun 08 2021
S4476 PCNA-I1 PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells. Jun 01 2021
S0841 OGG1-IN-08 OGG1-IN-08 (O8 OGG1 Inhibitor-Bio-X) is a potent inhibitor of 8-oxoguanine DNA glycosylase-1 (OGG1) with IC50 of 0.22 μM. OGG1-IN-08 decreases both the glycosylase and lyase activities of OGG1. May 24 2021
S6997 CHAPS CHAPS is a zwitterionic surfactant that decreases the sequence specificity of the nucleosome. Apr 27 2021
S5026 Irinotecan hydrochloride Irinotecan (CPT-11, (+)-Irinotecan) hydrochloride is an inhibitor of Topoisomerase I (Topo I) that exhibits cytotoxicity in LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. Apr 21 2021
S5195 Rucaparib Camsylate Rucaparib (Rubraca, AG014699, PF01367338) Camsylate 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. Apr 21 2021
S4447 Pipobroman Pipobroman (PB, Vercyte), a neutral amide of piperazine, acts as an alkylating agent with antiproliferative activity. Apr 13 2021
TGF-beta/smad
Catalog No. Product Name Information Added
S0069 VTX-27 VTX-27 (Compound 27) is a potent and selective inhibitor of protein kinase C θ (PKC θ) with Ki of 0.08 nM and 16 nM for PKC θ and PKC δ, respectively. Dec 08 2020
S0153 SJ000291942 SJ000291942 is a canonical bone morphogenetic proteins (BMP) signaling pathway activator. Oct 19 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
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
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
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
S7530 Vactosertib (TEW-7197) 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
S7208 Bisindolylmaleimide I (GF109203X) Bisindolylmaleimide I (GF109203X, GO 6850) 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
S6654 SRI-011381 SRI-011381 is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease. Jan 09 2020
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
GPCR & G Protein
Catalog No. Product Name Information Added
S6981 Glycerol phenylbutyrate Glycerol phenylbutyrate (GT4P, HPN-100M, Ravicti) is a nitrogen-binding agent and acts as a sigma-2 (σ2) receptor ligand with a pKi of 8.02. Glycerol phenylbutyrate is a prodrug in which phenylbutyrate (PBA) is released from the glycerol backbone by lipases in the gastrointestinal tract. Jul 16 2021
P1206 Tirzepatide (LY3298176) Tirzepatide (LY3298176, GIP/GLP-1 RA, TZP) is a dual GIP/GLP-1 receptor agonist. Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively. Jul 15 2021
S0326 Olodanrigan (EMA401) Olodanrigan (EMA401, PD-126055, (S) PD-126055) is a highly selective, orally active, peripherally restricted antagonist of angiotensin II type 2 receptor (AT2R). Olodanrigan (EMA401) analgesic action appears to involve the inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons. Jul 06 2021
S0193 TGR5 Receptor Agonist TGR5 Receptor Agonist (TGR5, CCDC, MDK00245, compd 6) is a potent agonist of TGR5(GPCR19, GPBAR1, M-BAR). TGR5 Receptor Agonist shows improved potency with pEC50 of 6.8 and 7.5 in the U2-OS cell assay and in melanophore cells, respectively. Jun 22 2021
P1203 Avexitide Avexitide (Exendin (9-39)) is a specific and competitive antagonist of glucagon-like peptide-1 (GLP-1) receptor. Jun 08 2021
S6347 5'-N-Ethylcarboxamidoadenosine (NECA) 5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5'-N-Ethylcarboxamidoadenosine acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway. Jun 07 2021
S0899 CPYPP CPYPP is an inhibitor of dedicator of cytokinesis 2 (DOCK2). CPYPP inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2DHR-2 for Rac1 in a dose-dependent manner with IC50 of 22.8 μM. CPYPP also inhibits DOCK180, DOCK5 and less DOCK9. Jun 01 2021
S7538 RS-102895 Hydrochloride RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively. May 24 2021
S0993 Remogliflozin etabonate (GSK189075) Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity inhibitor of sodium glucose cotransporter (SGLT2) with Ki of 1950 nM, 2140 nM, 43100 nM, 8570 nM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models. May 24 2021
S9851 PF-06882961 PF-06882961, a non-peptide agonist, activates the canonical G protein signaling activity only in the Glucagon-like peptide-1 (GLP-1) receptor with Trp33ECD. May 24 2021
PTK
Catalog No. Product Name Information Added
S6881 JND3229 JND3229 is a potent reversible inhibitor of EGFRC797S with an IC50 value of 5.8 nM. JND3229 also potently suppresses EGFRL858R/T790M and EGFRWT with IC50 values of 30.5 nM and 6.8 nM, respectively. Jul 16 2021
S7647 Lucitanib (E3810) hydrochloride Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively. Jun 28 2021
S6515 ALW II-41-27 ALW II-41-27 (compound 7) is a potent inhibitor of Eph receptor tyrosine kinase with Kd of 12 nM for EphA2. May 07 2021
S3187 SBI-477 SBI-477 is an insulin signaling inhibitor that deactivates the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain-containing 4 (ARRDC4). SBI-477 inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes. Apr 27 2021
S4967 Ceritinib dihydrochloride Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and STK22D with IC50 of 7 nM, 8 nM and 23 nM, respectively. Ceritinib exhibits antitomor activity. Apr 21 2021
S5190 Crizotinib hydrochloride Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. Apr 21 2021
S4947 Regorafenib Hydrochloride Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. Apr 13 2021
S9711 CH7233163 CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-tyrosine kinase with antitumor activities against tumor with EGFR-Del19/T790M/C797S. Apr 07 2021
S9786 BDTX-189 BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity. Mar 15 2021
S6839 MRX-2843 MRX-2843 (UNC2371) is an orally active dual inhibitor of tyrosine kinases MERTK and FLT3 with IC50 of 1.3 nM and 0.64 nM, respectively. Feb 08 2021
Epigenetics
Catalog No. Product Name Information Added
S9691 BMS-986158 BMS-986158 is a potent inhibitor of BET with IC50s of 6.6 nM and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively. Jul 16 2021
S8996 SNDX-5613 SNDX-5613 is a potent and selective inhibitor of menin-MLL binding with a Ki of 0.15 nM. SNDX-5613 shows anti-proliferative activity against multiple cell lines harboring MLLr translocations (MV4;11, RS4;11, MOLM-13, KOPN-8) with IC50 values ranging from 10-20 nM. Jul 16 2021
S9882 PFI-90

PFI-90 is a selective inhibitor of the histone demethylase KDM3B. PFI-90 induces apoptosis and cell differentiation resulting in delayed tumor progression in vivo.

Jul 15 2021
S9805 WM-3835 WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation. Jun 28 2021
S9667 CCS-1477 (CBP-IN-1) CCS1477(CBP-IN-1, CBP/p300-IN-4)is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc. Apr 27 2021
S3573 CC-90010 CC-90010 is a reversible, orally active and central nervous system-penetrant inhibitor of bromodomain and extra-terminal (BET) proteins. CC-90010 is applied in the study for advanced solid tumors. Apr 21 2021
S9685 GSK620 GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics. Mar 30 2021
S8665 GNE-781 GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity. Jan 25 2021
S9684 GSK046 GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET (bromodomain and extraterminal domain) with IC50 of 264 nM, 98 nM, 49 nM and 214 nM for BRD2BD2, BRD3BD2, BRD4BD2 and BRDTBD2, respectively. GSK046 exhibits immunomodulatory activity. Jan 05 2021
S7020 UNC0646 UNC0646 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 6 nM and 15 nM , respectively, with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity. Dec 23 2020
NF-κB
Catalog No. Product Name Information Added
S3384 (E/Z)-IT-603 (E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603. IT-603 is a NF-κB family member c-Rel inhibitor with an IC50 of 3 μM in electrophoretic mobility shift assay (EMSA). Jul 29 2021
S5899 (R)-(-)-Ibuprofen (R)-(-)-Ibuprofen ((R)-Ibuprofen) inhibits the activation of NF-κB in response to T-cell stimulation with IC50 of 121.8 μM. R(-)-ibuprofen exerts anti-inflammatory and antinociceptive effects. May 06 2021
S4611 TCEP Hydrochloride TCEP (Tris(2-carboxyethyl)phosphine) hydrochloride, a non-thiol reducing agent, promotes NF-κB-DNA binding in a dose-related manner. Apr 07 2021
S8935 BAY-985 BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM). Feb 09 2021
S1321 Urolithin B Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. Nov 18 2020
A2020 Denosumab (anti-RANK ligand) Denosumab (anti-RANK ligand) (AMG-162, Prolia, Xgeva) is a fully human monoclonal antibody that selectively inhibits primate RANKL. Denosumab inhibits the ability of human RANKL (143–317) to stimulate the formation of osteoclasts derived from murine RAW 264.7 cells with an IC50 value of 1.64 nM. Sep 15 2020
S8941 NIK SMI1 NIK SMI1 is a highly potent and selective NF-κB-inducing kinase (NIK) inhibitor with Ki of 0.23 nM for NIK-catalyzed hydrolysis of ATP to ADP. Aug 18 2020
S0507 CBL0137 CBL0137 (Curaxin-137) is an inhibitor of the histone chaperone FACT (facilitates chromatin transcription) that simultaneously suppresses NF-κB and activates p53 with EC50 of 0.47 μM and 0.37 μM, respectively. Jul 20 2020
S0425 TBK1/IKKε-IN-2 TBK1/IKKε-IN-2 (Ikk epsilon-in-1, IKKε-IN-1, MDK10496) is a dual inhibitor of TBK1 and IKKε. Jul 06 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
Metabolism
Catalog No. Product Name Information Added
S3486 AQX-016A AQX-016A is a potent agonist of SHIP1. AQX-016A inhibits DNFB induced inflammation in a mouse ear edema/cutaneous anaphylaxis model. Jul 29 2021
S6388 SHP099 SHP099 is a highly potent, selective and orally bioavailable small-molecule SHP2 inhibitor with an IC50  value of  71 nM and shows no activity against SHP1. Jul 28 2021
S9478 Trans-4-Phenyl-3-buten-2-one Trans-4-Phenyl-3-buten-2-one (trans-Benzylideneacetone, trans-Benzalacetone, trans-Benzylideneacetone) is an inhibitor of the enzyme phospholipase A2 (PLA2). Trans-4-Phenyl-3-buten-2-one is used as a flavouring agent, a fragrance and a bacterial metabolite. Jul 23 2021
S3483 TMP778 TMP778 is a selective inhibitor of RORγt with an IC50 of 5 nM in the Fluorescence Resonance Energy Transfer (FRET) assay and an IC50 of 17 nM in the RORγ assay. Jul 16 2021
S6895 TCPOBOP TCPOBOP is a constitutive androstane receptor (CAR) agonist. TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins. Jul 06 2021
S6391 Sephin-1 Sephin-1 (NSC-65390) is a selective inhibitor of a holophosphatase, a small molecule that safely and selectively inhibits a regulatory subunit of protein phosphatase 1 in vivo. Sephin-1 (NSC-65390) selectively bounds and inhibits the stress-induced PPP1R15A. Jul 06 2021
S6036 ER-000444793 ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening with IC50 of 2.8 μM. Jul 06 2021
S0286 AA26-9 AA26-9 is a potent and broad spectrum inhibitor of Serine hydrolases (SHs). Jun 28 2021
S9776 AG-636 AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity. Jun 28 2021
S2969 SR3335 SR3335 (ML-176) is a selective and inverse agonist of retinoic acid receptor-related receptor α (RORα) that directly binds to RORα with Ki of 220 nM. Jun 22 2021
Proteases
Catalog No. Product Name Information Added
S5960 Dabigatran etexilate mesylate Dabigatran etexilate mesylate (Pradaxa, BIBR 1048MS, Dabigatran etexilate methanesulfonate) is an orally active prodrug of Dabigatran which is a reversible and selective, direct thrombin inhibitor (DTI). Dabigatran selectively and reversibly inhibits human thrombin with Ki of 4.5 nM and thrombin-induced platelet aggregation with IC50 of 10 nM. Apr 27 2021
S4432 Ixazomib Citrate (MLN9708) Ixazomib citrate (MLN9708, Ninlaro) is a prodrug of Ixazomib (MLN2238), which is a selective, orally bioavailable inhibitor of 20S proteasome that inhibits the chymotrypsin-like proteolytic (β5) site with IC50 of 3.4 nM and Ki of 0.93 nM, respectively. Ixazomib (MLN2238) also inhibits caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31 nM and 3500 nM, respectively. Apr 13 2021
S0042 Fulacimstat Fulacimstat (BAY1142524) is an orally available inhibitor of chymase with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively. Mar 30 2021
S4426 Sacubitril hemicalcium salt Sacubitril (AHU-377) hemicalcium salt, a component of the heart failure medicine LCZ696, is a potent inhibitor of neprilysin (neutral endopeptidase, NEP). Mar 30 2021
S0479 ZK824859 ZK824859 is a potent, selective and orally bioavailable inhibitor of urokinase plasminogen activator (uPA) with IC50 of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively. Mar 15 2021
S3388 Sacubitrilat Sacubitrilat (Sac, LBQ-657) is an active inhibitor of neprilysin (NEP). Feb 09 2021
S3395 Tegobuvir Tegobuvir (TGV, GS 333126, GS-9190) is a non-nucleoside inhibitor of HCV RNA replication with proven antiviral activity in HCV-infected patients. Feb 09 2021
S2985 N-Acetyl-5-hydroxytryptamine

N-Acetyl-5-hydroxytryptamine (NAS, N-Acetylserotonin, Normelatonin, O-Demethylmelatonin), a precursor of melatonin, is a potent and selective agonist of TrkB receptor.

Dec 07 2020
S0341 T-26c T-26c is a highly potent and selective inhibitor of matrix metalloproteinase-13 (MMP-13) with IC50 of 6.9 pM, more than 2600-fold selectivity over other related metalloenzymes. Nov 17 2020
S7504 Salinosporamide A (NPI-0052) Salinosporamide A (NPI-0052, ML858, Marizomib, MRZ) is a novel marine derived proteasome inhibitor which inhibits CT-L β5, C-L β1, and T-L β2 proteasome activities in human erythrocyte-derived 20S proteasomes with IC50 of 3.5 nM, 430 nM, 28 nM. Nov 17 2020
Microbiology
Catalog No. Product Name Information Added
S7739 Telacebec (Q203) Telacebec (Q203, IAP6) is a novel antituberculosis drug that targets Mycobacterium tuberculosis cellular energy production through inhibition of the mycobacterial cytochrome bc1 complex. Telacebec (Q203, IAP6) is active against Mycobacterium tuberculosis H37Rv with MIC50 of 2.7 nM in culture broth medium. Jul 28 2021
S0754 Bisindolylmaleimide IV Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) is a potent inhibitor of protein kinase C (PKC) with IC50 of 0.55 μM. Bisindolylmaleimide IV also inhibits PKA with IC50 of 11.8μM. Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with IC50 of 0.2 μM. May 24 2021
S0081 DDD107498 DDD107498 (M-5717, DDD-498) is a P. falciparum translation elongation factor 2 inhibitor. DDD107498 exhibits a potent and novel spectrum of antimalarial activity against multiple life-cycle stages of the Plasmodium parasite. May 24 2021
S5235 Cefodizime Cefodizime (CEF, CDZ) is an aminothiazolyl cephalosporin with a broad spectrum of antibacterial activity. Apr 27 2021
S5979 2',3'-Dideoxyadenosine 2',3'-Dideoxyadenosine (ddA, ddAdo) is an anti-human immunodeficiency virus agent against human immunodeficiency virus (HIV) and human hepatitis B virus (HBV) replication. Apr 27 2021
S5330 Amikacin Sulfate Salt Amikacin (BAY 41-6551) sulfate, a semisynthetic analog of kanamycin, is an aminoglycoside antibiotic which is very active against most gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Apr 27 2021
S5961 Prednisolone disodium phosphate Prednisolone disodium phosphate (Hydeltrasol, Prednisolone 21-phosphate disodium) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties that exerts late mitogenic and biphasic effects on resistant acute lymphoblastic leukemia cells. Apr 27 2021
S5080 Neticonazole Neticonazole (SS717) is a selecvie inhibitor of exosome biogenesis and secretion. Neticonazole exhibits Neticonazole antifungal and antitumor activity. Apr 21 2021
S4974 Oxacillin sodium Oxacillin sodium (salt) is a narrow-spectrum β-lactam antibiotic that can be used for treatment of methicillin-sensitive Staphylococcus aureus (MSSA) bacteremia. Apr 13 2021
S5186 Cefpiramide Cefpiramide (Cefpiramide acid, Cefpiramido, Cefpiramidum, WY-44635, SM-1652) is a pseudomonas-active cephalosporin with a broad spectrum of antibacterial activity. Apr 13 2021
Apoptosis
Catalog No. Product Name Information Added
S6078 ICCB-19 hydrochloride ICCB-19 hydrochloride is an inhibitor of TNFRSF1A Associated Via Death Domain (TRADD) with IC50 of 1.12 μM and 2.01 μM for protecting Velcade-induced apoptosis in Jurkat cells and protecting RDA in MEFs, respectively. ICCB-19 indirectly inhibits Receptor-interacting serine/threonine-protein kinase 1 (RIPK1). ICCB-19 effectively induces autophagy. Jun 22 2021
S9840 SRS16-86 SRS16-86, a novel third-generation ferrostatin, is an inhibitor of ferroptosis. Jun 07 2021
S9733 Mito-TEMPO Mito-TEMPO (MT), a mitochondria-targeted superoxide dismutase mimetic, protects against the early phase of acetaminophen (APAP) hepatotoxicity by inhibiting peroxynitrite formation. Mito-TEMPO treatment inhibits APAP-induced RIP3 kinase expression. Jun 07 2021
S9839 SRS11-92 SRS11-92 (AA9), a Ferrostatin-1 (Fer-1) analogue, is a potent inhibitor of ferroptosis. SRS11-92 inhibits ferroptotic cell death induced by Erastin in HT-1080 human fibrosarcoma cells with EC50 of 6 nM. Jun 07 2021
S9817 Ac-FLTD-CMK Ac-FLTD-CMK is a specific inhibitor for inflammatory caspases. Ac-FLTD-CMK inhibits gasdermin D (GSDMD) cleavage by caspases-1, -4, -5, and -11 in vitro. Ac-FLTD-CMK is effective against caspases-1, caspases-4 and caspases-5 with IC50 of 46.7 nM, 1.49 μM and 329 nM, respectively. Jun 01 2021
S4613 Sodium Fluoride Sodium fluoride (NaF) induces apoptosis and autophagy via the endoplasmic reticulum (ER) stress pathway in MC3T3-E1 osteoblastic cells. May 09 2021
S0713 S107 hydrochloride S107 hydrochloride is a specific stabilizer of RyR2 (type 2 ryanodine receptor)/FKBP12.6 (FK506 binding protein 12.6) complex that affects Ca2+ signaling. Apr 21 2021
S5971 Pemetrexed Pemetrexed (LY231514, Alimta) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis. Apr 21 2021
S0931 Jaceosidin Jaceosidin, a flavonoid isolated from Artemisia vestita, possesses anti-tumor and anti-proliferative activities in many cancer cells. Jaceosidin induces apoptosis, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin inhibits COX-2 expression and NF-κB activation. Apr 13 2021
S3515 Benpyrine racemate Benpyrine racemate ((Rac)-Benpyrine) is a potent, highly specific and orally active inhibitor of TNF-α and attenuates TNF-α-induced inflammation, thereby reducing liver and lung injury. Apr 13 2021
MAPK
Catalog No. Product Name Information Added
S0542 R1487 R1487 is an orally bioavailable and highly selective inhibitor of p38α with an ic50 value of 10 nM. Jul 16 2021
S6930 MK2 Inhibitor III   Jul 15 2021
S4484 Trametinib DMSO solvate Trametinib (GSK1120212, JTP-74057, Mekinist) DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis. Apr 07 2021
S8569 KO-947 KO-947 is a potent and selective inhibitor of ERK1/2 kinases. KO-947 blocks ERK signaling and proliferation of tumor cells exhibiting dysregulation of MAPK pathway signaling at low nanomolar concentrations. Dec 08 2020
S0872 ASTX-029 ASTX-029 is an orally bioavailable inhibitor of the extracellular signal-regulated kinases (ERK) 1 and 2, with potential antineoplastic activity. ASTX-029 inhibits ERK-dependent tumor cell proliferation and survival. Nov 03 2020
S6905 MCP110 MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors. Sep 24 2020
S6882 HI-TOPK-032 HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells. Sep 24 2020
S6888 SEL201 SEL-201 (SLV-2436, SEL201-88) is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50 of 10.8  nM and 5.4 nM, respectively. Sep 10 2020
S9621 Donafenib (Sorafenib D3) Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively. Jul 20 2020
S8896 BAY-885 BAY-885 is a highly potent and selective ERK5 inhibitor. Jul 20 2020
Angiogenesis
Catalog No. Product Name Information Added
S6383 1-NM-PP1 1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively. Jun 15 2021
S6966 MT-802 MT-802 is a potent PROTAC that induces Bruton's tyrosine kinase (BTK) knockdown. MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. MT-802 has potential for treatment of C481S mutant chronic lymphocytic leukemia (CLL). Jun 01 2021
S4895 Nilotinib hydrochloride monohydrate Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition. Apr 07 2021
S4944 Fostamatinib disodium hexahydrate Fostamatinib (R788) disodium (Tamatinib Fosdium) hexahydrate, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM in a cell-free assay. Apr 07 2021
S8948 SRX3207 SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity. Mar 30 2021
S9715 Lanraplenib (GS-9876) Lanraplenib (GS-9876, GS-SYK) is a potent, highly selective and orally active inhibitor of Spleen Tyrosine Kinase (SYK) with IC50 of 9.5 nM. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. Feb 22 2021
S8351 PT2399 PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β. Dec 23 2020
S0373 CZC-8004 CZC-8004 (CZC-00008004) is a pan-kinase inhibitor that binds a range of tyrosine kinases including ABL kinase. Nov 27 2020
S1232 M1001 M1001 is a weak agonist of hypoxia-inducible factor-2α (HIF-2α) that binds to the HIF-2α PAS-B domain with Kd of 667 nM. Nov 18 2020
S1272 XL228 XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively. Nov 18 2020
Stem Cell & Wnt
Catalog No. Product Name Information Added
S5992 Heparan Sulfate Heparan sulfate (HS, Heparitin sulfate, Alpha-idosane, HHS 5, N-Acetylheparan Sulfate, Suleparoid, Tavidan), a constituent of HS proteoglycans (HSPGs), is a linear polysaccharide present on the cell surface. Heparan sulfate influences the binding affinity of intestinal epithelium cells (IECs) to Wnt, thereby promoting activation of canonical Wnt signaling and facilitating regeneration of small intestinal crypts after epithelial injury. May 17 2021
S9828 WAY-262611 WAY-262611 (BML-WN110, Compound 5) is a beta-catenin (β-Catenin) agonist that increases bone formation rate with EC50 of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also an inhibitor of dickkopf 1 (DKK1). May 06 2021
S0733 Tegatrabetan (BC-2059) Tegatrabetan (BC2059) is an antagonist of β-Catenin. Tegatrabetan (BC2059) treatment disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1) and proteasomal degradation and declines in the nuclear levels of β-catenin. Mar 08 2021
S6961 Foxy-5 Foxy-5, a Wnt-5a mimicking hexapeptide, is a WNT signalling pathway modulator potentially for the treatment of metastatic breast cancer, prostate cancer and colorectal cancer. Jan 11 2021
S2962 NP-G2-044 NP-G2-044 is a potent, orally active inhibitor of the actin-bundling activity of fascin with IC50 of ~0.2 μM. NP-G2-044 blocks tumor metastasis and increases antitumor immune response. Nov 30 2020
S6901 MSAB MSAB is a selective inhibitor of Wnt/β-catenin signaling that binds to β-catenin, promoting its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB shows potent anti-tumor effects. Nov 27 2020
S8968 PRI-724 PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP. Aug 24 2020
S7981 CCT251545 CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. Aug 18 2020
S0458 KY1220 KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells. Jul 14 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
Ubiquitin
Catalog No. Product Name Information Added
S6883 HBX 19818 HBX19818 is a specific inhibitor of USP7 with an IC 50 of 28.1 μM. Jul 23 2021
S2881 Homo-PROTAC cereblon degrader 1 Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3. Jul 06 2021
S4453 NPD8733 NPD8733 is an inhibitor of cancer cell-enhanced fibroblast migration that specifically binds to valosin-containing protein (VCP)/p97, a member of the ATPase-associated with diverse cellular activities (AAA+) protein family. Jun 15 2021
S0322 BC-1215 BC-1215 is an inhibitor of F-box protein 3 (Fbxo3, a ubiquitin E3 ligase component) with IC50 of 0.9 μg/mL and LC50 of 87 μg/ml for IL-1β release. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6. Jun 01 2021
S8967 XL177A XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM. May 24 2021
S9724 SZL P1-41 SZL P1-41 (compound #25) is a specific inhibitor of S-phase kinase-associated protein 2 (Skp2) that indeed binds to Skp2, prevents Skp2-Skp1 interaction and inhibits Skp2 SCF E3 ligase activity, which consequently suppresses survival of cancer cells and cancer stem cells. SZL P1-41 causes higher apoptosis rates in cancer cells. Apr 27 2021
S3502 (S,R,S)-AHPC-PEG4-NH2 hydrochloride (S,R,S)-AHPC-PEG4-NH2 hydrochloride (VH032-PEG4-NH2 hydrochloride, VHL Ligand-Linker Conjugates 4 hydrochloride, E3 ligase Ligand-Linker Conjugates 7) is a PROTAC E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker. Feb 08 2021
S8697 ML792 ML-792 is a potent and selective inhibitor of SUMO (small ubiquitin-like modifier)-activating enzyme (SAE). ML-792 inhibits SAE/SUMO1 and SAE/SUMO2 in ATP–inorganic pyrophosphate (PPi) exchange assays with IC50 of 3 nM and 11 nM, respectively. Jan 05 2021
S0515 PLpro inhibitor  PLpro inhibitor (compound 6) is a potent papain-like protease (PLpro)/deubiquitinase (DUBs) inhibitor with IC50 of 2.6 μM and EC50 of 13.1 μM that blocks SARS virus replication. Dec 29 2020
S8849 TAS4464 TAS4464 is a potent and highly selective NEDD8 activating enzyme (NAE) inhibitor with IC50 of 0.955 nM. TAS4464 exhibits superior antitumor activity with prolonged target inhibition. Dec 29 2020
Neuronal Signaling
Catalog No. Product Name Information Added
S6985 Varenicline Varenicline is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). Varenicline also acts as an agonist of 5-HT3 serotonine receptors. Jul 26 2021
S0446 TCN 201 TCN-201 is a selective GluN1/GluN2A (NR1/NR2A) NMDA receptor antagonist with pIC50 6.8 for NR1/NR2A and <4.3 for NR1/NR2B (GluN1/GluN2B),respectively. Jul 23 2021
S6853 ONC206 ONC206 is a selective antagonist of dopamine D2-like receptors (DRD2/3/4) with broad-spectrum anti-tumor activity. May 24 2021
S4358 Pimozide Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity. May 24 2021
S3520 AZ10606120 dihydrochloride AZ10606120 dihydrochloride (2HCl) is a potent and selective antagonist for P2X7 receptor (P2X7R) with IC50 of ~10 nM. AZ10606120 dihydrochloride exhibits anti-depressant effects and reduces tumour growth. May 18 2021
S4359 Carbamoylcholine chloride (Carbachol) Carbamoylcholine chloride (Carbachol, Carbamylcholine chloride, Carbastat, Miostat) is a cholinergic agonist that mimics the effect of acetylcholine on both the muscarinic and nicotinic receptors. May 10 2021
S0717 Varenicline (CP 526555) dihydrochloride Varenicline (CP 526555, Chantix, Champix) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation. May 07 2021
S3913 Pimethixene maleate Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively. Apr 27 2021
S5770 Pizotifen Pizotifen (Pizotyline, BC-105) is a potent antagonist of 5-Hydroxytryptamine (5-HT, Serotonin) 5-HT2 receptor with a high affinity for 5-HT1C binding site. Apr 27 2021
S9789 JHU37152 JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively. Apr 27 2021
Others
Catalog No. Product Name Information Added
A2117 Mouse IgG2a isotype control-InVivo Mouse IgG2a isotype control-InVivo (Clone:C1.18.4) monoclonal antibody is ideal for use as a non-reactive isotype-matched control for mouse IgG2a antibodies in most in vivo and in vitro applications. Jul 29 2021
S0358 GSK4716 GSK4716 is a selective agonist of Estrogen-Related Orphan Nuclear Receptors ERR and ERRγ with an IC50 of 2 µM in the ERRγ FRET assay. Jul 29 2021
S5984 AST5902 trimesylate AST5902 is the principal metabolite of alflutinib both in vitro and in vivo, which exerts remarkable antineoplastic activity similar to alflutinib. AST5902 exhibits much weak CYP3A4 induction potential compared to alflutinib. Jul 29 2021
S6954 CK-869 CK-869 (CK 0157869) is a small molecule inhibitor of actin-related protein 2/3 (Arp2/3) complex with an IC50 of 7 μM. CK-869 can directly suppresses microtubule assembly both in vitro and in vivo. Jul 28 2021
S9729 Visomitin (SKQ1) Visomitin (SKQ1) is a novel mitochondrial-targeted antioxidant that holds promise in the treatment of inflammation associated with ocular surface diseases such as dry eye disease (DED) and corneal wounds. SkQ1 shows a TC50 of 317 nM on HCjE cells. Jul 28 2021
S6928 Fluorescein-5-isothiocyanate (FITC) Fluorescein-5-isothiocyanate (FITC, Fluorescein isothiocyanate isomer I, 5-FITC) is a fluorescent probe capable of being conjugated to tissue and proteins. Jul 28 2021
S6953 GW406108X GW406108X (GW108X) is an inhibitor of Kif15 (Kinesin-12) with an IC50 of 0.82 μM in the ATPase assay. GW406108X inhibits recombinant ULK1 kinase activity with a pIC50 of 6.37 and blocks autophagy in cells, without affecting the upstream signalling kinases mTORC1 and AMPK. Jul 26 2021
S9900 JNJ-63576253 (TRC-253) JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM. JNJ-63576253 displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer. Jul 26 2021
S9775 SCR130 SCR130 is a novel DNA repair inhibitor with IC50s of 14 μM in Reh cells and 2 μM in Nalm6 cells. SCR130 specifically inhibits DNA Ligase IV‐mediated joining with minimal or no effect on Ligase III and Ligase I mediated joining. Jul 26 2021
S9885 MYLS22 MYLS22 is a first-in-class and selective inhibitor of optic atrophy 1 (OPA1) with anti-angiogenesis and anti-cancer activity. Jul 23 2021