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PI3K/Akt/mTOR
Catalog No. Product Name Information Added
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
S9695 iHAP1 iHAP1 is an activator of protein phosphatase 2A (PP2A) enzymes that activates PP2A-B56ε and potently kills malignant cells. Nov 27 2020
S6517 GNE-493 GNE-493 (compound 5) is a potent, selective and orally available dual inhibitor of pan-PI3-kinase and mTOR with IC50 of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. Nov 27 2020
S0148 HAMNO HAMNO (NSC-111847) is a potent and selective replication protein A (RPA) inhibitor with anti-tumor activity. HAMNO inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR. Nov 24 2020
S1323 7-Methoxyisoflavone 7-Methoxyisoflavone (MIF) is a potent activator of adenosine monophosphate-activated protein kinase (AMPK). Nov 18 2020
S0983 JX06 JX06 as a selective covalent inhibitor of PDK1 in cells. JX06 dose-dependently inhibits PDK1, PDK2 and PDK3 with IC50 0.049 μM, 0.101 μM and 0.313 μM, respectively. Nov 09 2020
S0385 S6K-18 S6K-18 is a highly selective inhibitor of ribosomal protein S6 kinase beta-1 (S6K1, p70S6K, p70-S6K). Nov 09 2020
S6912 Vacuolin-1 Vacuolin-1 is a potent and cell-permeable inhibitor that blocks the Ca(2+)-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. Vacuolin-1 is also a potent and selective PIKfyve inhibitor, and inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition. Nov 03 2020
S0795 O-304 O-304 (O-304X) is an orally available pan-activator of AMPK activated protein kinase (AMPK). O-304 (O-304X) exhibits a great potential as a novel drug to treat type 2 diabetes (T2D) and associated cardiovascular complications. Nov 03 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
S0706 ISRIB ISRIB is an integrated stress response (ISR) inhibitor that potently reverses the effects of eukaryotic initiation factor 2α (eIF2α) phosphorylation with IC50 of 5 nM. Feb 09 2021
S0890 MLS000532223 MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases with EC50 ranging from 16 μM to 120 μM. Dec 29 2020
S0780 Oncrasin-1 Oncrasin-1 (Onc-1) is a potent RNA polymerase II inhibitor with antitumor activity that kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells. Dec 23 2020
S6963 APTO-253

APTO-253 (LOR-253, LT-253) inhibits c-Myc expression and selectively induces CDKN1A (p21), promotes G0-G1 cell-cycle arrest, and triggers apoptosis in acute myeloid leukemia (AML) cells. APTO-253 is also an inducer of KLF4 (Krüppel-like factor 4).

Dec 15 2020
S0354 Alsterpaullone Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders. Dec 08 2020
S8782 LY3295668 LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively. Nov 27 2020
S8863 YKL-5-124 YKL-5-124 is a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for inhibiting CDK7/Mat1/CycH, CDK2 and CDK9 respectively. It displays biochemical and cellular selectivity for CDK7 over CDK12/13. Nov 27 2020
S2942 EB-3D EB-3D is a potent and selective inhibitor of choline kinase α (ChoKα) with IC50 of 1 μM for ChoKα1. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. Nov 17 2020
S8389 Trilaciclib Trilaciclib (G1T28, G1T28-1) is a highly potent, selective and reversible cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. Trilaciclib inhibits CDK4/cyclin D1 and CDK6/cyclin D3 with IC50 of 1 nM and 4 nM, respectively. Nov 09 2020
S8214 Empesertib (BAY1161909) Empesertib (BAY1161909, Mps1-IN-5), a derivative of triazolopyridine, is an orally bioavailable, selective inhibitor of the serine/threonine monopolar spindle 1 (Mps1) kinase with IC50 of <1 nM. Empesertib has potential antineoplastic activity. Nov 03 2020
DNA Damage
Catalog No. Product Name Information Added
S0864 ACY-775 ACY-775 is a potent and selective histone deacetylase 6 (HDAC6) inhibitor with IC50 of 7.5  nM. Jan 18 2021
P1202 TMPyP4 tosylate

TMPyP4 tosylate (TMP 1363), a quadruplex-specific ligand, inhibits the interaction between G-quadruplex (G4) and IGF-1 (Insulin-like growth factor type I). TMPyP4 tosylate is also a telomerase inhibitor with antitumor effects.

Jan 04 2021
S8844 BRD0539 BRD0539 is a potent inhibitor of Streptococcus pyogenes Cas9 (SpCas9) with IC50 of 22 μM in an in vitro DNA cleavage assay. Dec 29 2020
S6958 Treosulfan

Treosulfan (NSC 39069, Treosulphan) is an alkylating agent used for conventional and high-dose chemotherapy regimens. Treosulfan is potently cytotoxic against pancreatic cancer cell lines.

Dec 22 2020
S9712 Fluzoparib (SHR-3162)

Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity.

Dec 15 2020
S0063 RG3039 RG3039 (PF-06687859, PF 6687859, Quinazoline 495) is an orally bioavailable and brain-penetrant inhibitor of the mRNA decapping enzyme DcpS with IC50 of 4.2 nM and IC90 of 40 nM, respectively. Nov 30 2020
S0816 Brr2 Inhibitor C9 Brr2 inhibitor C9 (Brr2 Inhibitor 9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa a group of progressive retinal degenerative disorders. Nov 24 2020
S9718 TK216

TK216 is a potent inhibitor targeting E26 transformation specific (ETS) factors via blocking the protein-protein interaction with RNA helicases. TK216 exhibits antilymphoma activity.

Nov 23 2020
S1313 GSK3117391 GSK3117391 (GSK3117391A, HDAC-IN-3) is a potent histone deacetylase (HDAC) inhibitor. Nov 18 2020
S8586 Nedisertib (M3814) Nedisertib (M3814, Peposertib, MSC2490484A) is an orally bioavailable, highly potent and selective inhibitor of DNA activated protein kinase (DNA-PK) with IC50 of < 3 nM. Nov 17 2020
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 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
S2945 SCH-442416 SCH-442416 is a selective antagonist of adenosine A2A receptor that binds to human and rat adenosine A2A receptors with Ki of 0.048 nM and 0.5 nM, respectively. Feb 23 2021
S9693 Vericiguat Vericiguat (BAY1021189, Verquvo) is a potent, orally available and soluble guanylate cyclase (sGC) stimulator. Feb 09 2021
S9744 AZ3451 AZ3451 is a potent antagonist of protease-activated receptor 2 (PAR2) that binds to a remote allosteric site outside the helical bundle with IC50 of 23 nM. Feb 08 2021
S3479 R243 R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis. Feb 02 2021
S0034 BAR501 BAR501 is a potent and selective G protein-coupled bile acid receptor 1 (GPBAR1, GPCR19, TGR5) agonist that effectively transactivates GPBAR1 in HEK293 cells overexpressing a CRE along with GPBAR1 with EC50 of 1 μM. Jan 05 2021
S9743 Ciliobrevin D Ciliobrevin D (compound 5) is a cell-permeable, reversible and specific antagonist of AAA+ (ATPases associated with diverse cellular activities) ATPase motor cytoplasmic dynein. Ciliobrevin D perturbs primary cilia formation and blocks Hedgehog (Hh) signaling. Dec 28 2020
S0869 Carbetapentane Carbetapentane (Pentoxyverine, CB) is an antitussive anticonvulsant nonselective sigma-1 (σ1) agonist. Dec 15 2020
S0851 G-1 G-1 is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM. Dec 15 2020
S0772 L-732138 L-732138 (L-732,138) is a selective, potent and competitive antagonist of neurokinin-1 (NK-1) receptor/substance P (SP) receptor. L-732138 inhibits the binding of 125I-SP to the human NK-1 receptor stably expressed in CHO cells with IC50 of 2.3 nM. Nov 24 2020
S6950 PRE-084 hydrochloride PRE-084 hydrochloride (HCl) is a potent, selective sigma-1 receptor (σ1, S1R) agonist with IC50 of 44 nM in the sigma receptor assay. Nov 18 2020
PTK
Catalog No. Product Name Information Added
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
S5860 Larotrectinib Larotrectinib (Vitrakvi, LOXO-101, ARRY-470) is an ATP-competitive, oral administered and highly selective inhibitor of the tropomyosin-related kinase (TRK) family receptors. Feb 08 2021
S0711 Canertinib dihydrochloride Canertinib (CI-1033, PD-183805, compound 18) dihydrochloride is a potent and irreversible inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. Canertinib dihydrochloride inhibits cellular EGFR and ErbB2 autophosphorylation with IC50 of 7.4 nM and 9 nM, respectively. Jan 26 2021
S8920 JBJ-04-125-02 JBJ-04-125-02 is a mutant-selective allosteric inhibitor of EGFR. Jan 26 2021
S0012 E260 E260 (Fer and FerT inhibitor E260) is a Fer kinase and FerT inhibitor that selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level. Jan 05 2021
S0290 SU5204 SU5204 is a tyrosine kinase inhibitor with IC50 of 4 μM and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively. Dec 29 2020
S0504 SU14813 SU14813 (SU 014813) is a multiple receptor tyrosine kinase inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit). SU14813 exhibits potent antiangiogenic and antitumor activity. Dec 15 2020
S0827 LM22A-4 LM22A-4 (LM 22A4) is a specific agonist of tyrosine kinase receptor B (TrkB) that reduces the development of tissue injury associated with spinal cord trauma. Nov 27 2020
S8833 TAS0728 TAS0728 (TPC 107) is a potent, selective, orally active, irreversible and covalent-binding inhibitor of HER2 (human epidermal growth factor receptor 2) with IC50 of 13 nM. TAS0728 inihibits BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2 with IC50 of 4.9 nM, 8.5 nM, 31 nM, 65 nM, 33 nM, 25 nM, 86 nM and 36 nM, respectively. TAS0728 shows antitumor activity. Nov 27 2020
S0540 BAY-474 BAY-474 is an inhibitor of tyrosine-protein kinase c-Met and can act as an epigenetics probe. Nov 24 2020
Epigenetics
Catalog No. Product Name Information Added
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
S8934 VTP50469 VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity. Dec 15 2020
S1027 FL-411 FL-411 (BRD4-IN-1) is a potent and selective inhibitor of Bromodomain-containing protein 4 (BRD4) with IC50 of 0.43 μM for BRD4(1). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction. Nov 30 2020
S1161 Histone Acetyltransferase Inhibitor II

Histone Acetyltransferase Inhibitor II (HAT Inhibitor II, compound 2c) is a potent, selective and cell-permeable p300 histone acetyltransferase (HAT) inhibitor with IC50 of 5 μM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.

Nov 27 2020
S0344 Y06036 Y06036 (Compound 6i) is a potent and selective inhibitor of BET with antitumor activity. Y06036 binds to the BRD4(1) bromodomain with Kd of 82 nM. Nov 24 2020
S7868 S-Adenosyl-L-homocysteine (SAH) S-Adenosyl-L-homocysteine (SAH, S-Adenosylhomocysteine, AdoHcy, Formycinylhomocysteine) is an inhibitor for (Methyltransferase Like 3-14) METTL3-METTL14 heterodimer complex (METTL3-14) with IC50 of 0.9 μM. Nov 24 2020
S9659 UNC6852 UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. UNC6852 is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL. Nov 24 2020
S1325 L-2-Hydroxyglutaric acid disodium

L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation. L-2-Hydroxyglutaric acid disodium is also an inhibitor of mitochondrial creatine kinase (Mi-CK) with Km and Ki of 2.52 mM and 11.13 mM, respectively.

Nov 23 2020
NF-κB
Catalog No. Product Name Information Added
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
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
S6671 SN50 SN50 (NF-κB 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
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
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
S7352 Bay 11-7085 BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM. May 07 2019
Metabolism
Catalog No. Product Name Information Added
S0820 RP-64477 RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT). RP-64477 inhibits ACAT activity with IC50 of 113 nM, 503 nM, and 180 nM in human intestinal (CaCo-2), hepatic (HepG2) and monocytic (THP-1) cell assays, respectively. Feb 23 2021
S9678 AT-56 AT-56 is an orally active and selective inhibitor of lipocalin-type prostaglandin (PG) D synthase (L-PGDS) with Ki of 75 μM and IC50 of 95 μM. Feb 23 2021
S8052 LY-2183240 LY-2183240 is a potent, covalent inhibitor of the EC-degrading enzyme fatty acid amide hydrolase (FAAH). LY-2183240 disrupts the cellular uptake of the lipid endocannabinoid (EC) anandamide and promote analgesia in vivo. LY-2183240 is also an inhibitor of monoacylgylcerol lipase (MGL). Feb 23 2021
S9742 Indisulam Indisulam (E7070), a sulfonamide anticancer agent, is a potent carbonic anhydrase (CA) inhibitor that inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Indisulam suppresses the expression of cyclin E and phosphorylation of CDK2, both of which are essential for the G1 to S transition. Feb 08 2021
S9794 Melittin Melittin (MLT, Forapin, Forapine) is an activator of phospholipase A2 (PLA2) that stimulates the activity of the low molecular weight PLA2, while it does not the increase the activity of the high molecular weight enzyme. Feb 08 2021
S0316 MPO-IN-28 MPO-IN-28 (Compound 28) is an inhibitor of myeloperoxidase (MPO) with IC50 of 44 nM. Feb 02 2021
S8910 OSMI-4 OSMI-4 is an inhibitor of O-GlcNAc transferase (OGT) with EC50 of 3 μM in cells. Feb 02 2021
S0522 CM10 CM10 is a potent and selective inhibitor of aldehyde dehydrogenase 1A family (ALDH1A) with IC50 of 1700 nM, 740 nM and 640 nM for ALDH1A1, ALDH1A2 and ALDH1A3, respectively. CM10 exhibits anti-cancer activity. Jan 26 2021
S9783 6-Aminonicotinamide 6-Aminonicotinamide (6AN) is an antimetabolite used to inhibit the NADPH-producing pentose phosphate pathway (PPP) in many cellular systems, making them more susceptible to oxidative stress. 6-Aminonicotinamide is a competitive inhibitor of NADP+-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) with Ki of 0.46 μM. Jan 18 2021
S0170 BMS-687453 BMS-687453 (compound 2) is a potent and selective agonist of PPARα with EC50 of 10 nM and IC50 of 260 nM for human PPARα. Jan 18 2021
Proteases
Catalog No. Product Name Information Added
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
S6929 Dextran sulfate sodium (DSS) Dextran sulfate sodium (DSS) is a potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) in vitro that inhibits virus adsorption to the host cells. Nov 03 2020
S3309 Solasodine Solasodine (Purapuridine, Solancarpidine, Solasodin, Salasodine, Salasdine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine reduces the mRNA level of matrix metalloproteinase-2 (MMP-2), MMP-9 and extracellular inducer of matrix metalloproteinase (EMMPRIN), but increases the expression of reversion-inducing cysteine-rich protein with kazal motifs (RECK). Solasodine downregulates oncogenic microRNA-21 (miR-21), which has been known to target RECK. Solasodine also reduces PI3K/Akt signaling pathways and downregulates expression of miR-21. Oct 26 2020
S7394 MDL-28170 MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase. Sep 02 2020
S9641 Pibrentasvir (ABT-530) Pibrentasvir (ABT-530) is a novel and pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with EC50 ranging from 1.4 pM to 5.0 pM against HCV replicons containing NS5A from genotypes 1 to 6. Sep 02 2020
S8966 T-5224 T-5224 is a selective inhibitor of transcription factor c-Fos/activator protein (AP)-1 with anti-inflammatory effects. T-5224 specifically inhibits the DNA binding activity of c-Fos/c-Jun and the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription. Aug 18 2020
Microbiology
Catalog No. Product Name Information Added
S0235 Lavendustin B Lavendustin B inhibits HIV-1 integrase (IN) interaction with its cognate cellular cofactor lens epithelium-derived growth factor (LEDGF/p75). Lavendustin B is an inhibitor of Tyrosine Kinase and also a competitive inhibitor of glucose transporter 1 (Glut1). Feb 09 2021
S3218 Amiloxate Amiloxate (Amiloxiate, Isoamyl Methoxycinnamate, Isopentyl 4-methoxycinnamate, Isoamyl 4-methoxycinnamate, Isoamyl p-methoxycinnamate, Isopentyl p-methoxycinnamate) is EMA-approved chemical UV-filter used in cosmetics. Amiloxate is a cinnamic acid derivative with anti-inflammatory activity. Oct 12 2020
S0833 EIDD-1931 EIDD-1931 (Beta-d-N4-hydroxycytidine, β-d-N4-hydroxycytidine, NHC) is an active metabolite of EIDD-2801, a promising COVID-19 inhibitor. EIDD-1931 (NHC) has broad spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and related zoonotic group 2b or 2c Bat-CoVs with average IC50 of 0.15 μM, as well as increased potency against a coronavirus bearing resistance mutations to the nucleoside analog inhibitor remdesivir. Aug 10 2020
S6867 Glyceryl monocaprate (Monocaprin) Monocaprin (Glyceryl caprate) is a 1-monoglyceride of capric acid that has antimicrobial activity against enveloped viruses, certain bacteria, and the yeast Candida albicans. Aug 04 2020
S2764 DTNB DTNB (Ellman’s Reag, Ellmans Reagenz, 5,5′-Dithiobis(2-nitrobenzoic acid), 5,5′-Dithiobis-2-nitrobenzoesäure) is a non-fluorescent probe used to quantify the number or concentration of thiol groups in a sample. DTNB is also an allosteric inhibitor of dengue virus protease (NS2B-NS3pro) and Streptomyces proteases. Aug 04 2020
S6801 AKOS B018304 AKOS B018304, an arylalkylidene derivative with polar substitution at para-position, is a potent inhibitor of chikungunya virus with low micro molar activity. Jul 28 2020
S0076 ABX464 ABX464 (SPL-464) is a novel anti-HIV molecule that inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) from 5 different donors with IC50 ranging between 0.1 μM and 0.5 μM. Jul 20 2020
S6848 3'-Fluoro-3'-deoxythymidine (Alovudine) 3'-Fluoro-3'-deoxythymidine (Alovudine, CL 184824, FddThd, FLT, MIV-310) 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
S4307 Auranofin Auranofin (Ridaura, 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
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
Apoptosis
Catalog No. Product Name Information Added
S8924 DT2216 DT2216 is a potent and selective degrader of BCL-XL based on PROTAC technology. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. Jan 26 2021
S3231 UCB-9260 UCB-9260 is an orally active inhibitor that inhibits TNF signalling by stabilising an asymmetric form of the trimer. UCB-9260 binds TNF with Kd of 13  nM. UCB-9260 also inhibits NF-κB with IC50 of 202 nM after TNF stimulation. Jan 18 2021
S0323 Antineoplaston A10 Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis. Dec 23 2020
S6957 β-Elemene

β-Elemene ((-)-β-Elemene, Levo-β-elemene) is a sesquiterpene compound extracted from the herb Curcuma Rhizoma with antitumor activities. β-elemene can inhibit cell proliferation, arrest the cell cycle, and induce cell apoptosis or autophagy.

Dec 22 2020
S0067 GS-444217 GS-444217 (ASK1-IN-1) is a potent, selective, orally available and ATP-competitive inhibitor of ASK1 (apoptosis signal-regulating kinase 1) with IC50 of 2.87 nM. Dec 15 2020
S6962 TPEN

TPEN (TPEDA) is a specific cell-permeable heavy metal chelator that induces apoptosis in NB4 cells via negatively regulating intracellular NO and Zn2+ signaling. TPEN (TPEDA) may be a potential therapeutic strategy for APL (acute promyelocytic leukemia).

Dec 15 2020
A2015 Avelumab (anti-PD-L1) Avelumab (anti-PD-L1) (Bavencio, MSB0010718C) is a fully human IgG1 monoclonal antibody that targets the protein programmed death-ligand 1 (PD-L1). Avelumab exhibits potential antibody-dependent cell-mediated cytotoxicity and is used for the treatment of several kinds of carcinoma. MW=143.8 kDa. Dec 08 2020
S7100 WEHI-539 HCl WEHI-539 HCl (WEHI-539 hydrochloride) has high affinity (IC50=1.1 nM) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. It has more than a 400-fold higher affinity for BCL-XL versus other prosurvival BCL-2 family members. Nov 27 2020
S8831 MRTX-1257 MRTX-1257 is a potent, selective, irreversible, covalent and orally active inhibitor of KRAS G12C with IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. Nov 24 2020
S0431 ML281 ML281 is a potent and selective inhibitor of Serine/threonine kinase 33 (STK33) with IC50 of 0.014 μM. ML281 is selectively toxic to KRAS-dependent cancer cell lines. Nov 17 2020
MAPK
Catalog No. Product Name Information Added
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
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
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
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
Angiogenesis
Catalog No. Product Name Information Added
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
S2937 SYP-5 SYP-5 is an inhibitor of Hypoxia-inducible factor-1 (HIF-1) that suppresses tumor cell migration and invasion, as well as tumor angiogenesis. Nov 17 2020
S9643 DGY-06-116 DGY-06-116 is an irreversible covalent and selective inhibitor of Src with IC50 of 2.6 nM. Nov 03 2020
S0729 TP0463518 TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with Ki of 5.3 nM for human PHD2. TP0463518 inhibits human PHD1, human PHD3 and monkey PHD2 with IC50 of 18 nM, 63 nM and 22 nM, respectively. Oct 26 2020
S9699 Desidustat Desidustat (ZYAN1, ZYAN1-1001), an antianaemic drug candidate, is an orally active hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor (HIF-PHI) that stimulates erythropoiesis. Oct 19 2020
S9656 Enarodustat (JTZ-951) Enarodustat (JTZ-951) is a potent and orally active HIF prolyl hydroxylase inhibitor with IC50 of 0.22 μM for PHD2 and EC50 of 5.7 μM for EPO release from Hep3B cells. Enarodustat has the potential for the treatment of renal anemia. Oct 13 2020
Stem Cell & Wnt
Catalog No. Product Name Information Added
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
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
S1146 Cyclopamine Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells. Dec 19 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
Ubiquitin
Catalog No. Product Name Information Added
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
S8829 TAK-981 TAK-981 is a novel, selective inhibitor of the SUMOylation enzymatic cascade with potential immune-activating and antineoplastic activities. Nov 03 2020
S6933 GEN-6776 GNE-6776 is a potent, non-covalent, selective and orally bioavailable inhibitor of USP7 with IC50 of 1.34 μM and 0.61 μM for full length USP7 and USP7 catalytic domain, respectively. Nov 03 2020
S0884 RA-9 RA-9 is a cell-permeable, potent and selective inhibitor of proteasome-associated deubiquitinating enzymes (DUBs) with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines. Oct 19 2020
S9605 Apcin Apcin (APC inhibitor) is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C) that binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates. Sep 25 2020
S0309 COH000 COH000 is an allosteric, covalent and irreversible ubiquitin-like 1-activating enzyme (SUMO-activating enzyme / E1) inhibitor with IC50 of 0.2 μM for SUMOylation in vitro. Aug 24 2020
S6878 GSK2643943A GSK2643943A is an inhibitor of deubiquitylating enzyme (DUB) with IC50 of 160 nM for USP20/Ub-Rho. Aug 24 2020
Neuronal Signaling
Catalog No. Product Name Information Added
S0826 A-740003 A-740003 is a potent, selective and competitive antagonist of P2X7 receptor with IC50 of 18 nM and 40 nM for rat and human P2X7 receptors, respectively. A-740003 potently blocks agonist-evoked IL-1β release and pore formation with IC50 of 156 nM and 92 nM in differentiated human THP-1 cells. Nov 27 2020
S0766 RHC 80267 RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC). Nov 27 2020
S9686 NBQX (FG9202) NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect. Nov 24 2020
S9719 CB-103

CB-103 is an orally active inhibitor of the Notch transcription activation complex. CB-103 produces Notch loss-of-function phenotypes in flies and mice and inhibits the growth of human breast cancer and leukemia xenografts.

Nov 23 2020
S0165 Ampalex (CX-516) Ampalex (CX-516, Ampakine CX 516, BDP-12, SPD 420) is a positive allosteric modulator of AMPA receptor. Ampalex exhibits potential treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI). Nov 17 2020
S0486 Hoechst 34580 Hoechst 34580 (HOE 34580) is a cell-permeable blue fluorescent dye to stain DNA and nuclei. Hoechst 34580 is also a good candidate for treating the Alzheimer's disease by inhibiting amyloid beta (Aβ) formation with IC50 of 0.86 μM. Nov 17 2020
S0552 BNC210 BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR). Nov 09 2020
S0782 VU0238441 VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50 of 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and >10 μM for M5, M3, M2, M1 and M4, respectively. Nov 09 2020
S0783 VU0119498 VU0119498 is a pan Gq muscarinic acetylcholine receptor (mAChR) M1, M3, M5 positive allosteric modulator (PAM) with EC50 of 6.1 μM, 6.4 μM, 4.1 μM, respectively. Nov 09 2020
S0496 PF-04995274 PF-04995274 (PF-4995274) is a potent, high-affinity, orally active and partial agonist of serotonin 4 receptor (5-HT4R) with EC50 of 0.47 nM, 0.36 nM, 0.37 nM and 0.26 nM for human 5-HT4A/4B/4D/4E, respectively. As for rat 5-HT4S/4L/4E, the EC50 is 0.59 nM, 0.65 nM and 0.62 nM, respectively. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease. Nov 03 2020
Others
Catalog No. Product Name Information Added
S9609 SAR439859 SAR439859 (compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation. Feb 09 2021
S3415 AA92593 AA92593 is a selective antagonist of Melanopsin (OPN4) which is a photo-pigment found in a small subset of intrinsically photosensitive ganglion cells (ipRGCs) of the mammalian retina. Feb 09 2021
S3497 Gadobutrol Gadobutrol (Gadovist, Gadavist) is a non-ionic macrocyclic gadolinium-based contrast agent (GBCA) that is usedfor tissue contrast enhancement in magnetic resonance imaging (MRI). Feb 01 2021
S3498 Ecamsule.2Na Ecamsule.2Na is the Sodium salt form of Ecamsule. Ecamsule is an active ingredient of sunscreens that protects the skin from sunburn and erythema. Feb 01 2021
S3505 Polidocanol Polidocanol (Polyoxyethylene lauryl ether, Polyoxyethyleneglycol Dodecyl Ether, Brij30, Laureth-23, Varithena) is a sclerosant used for treating uncomplicated spider veins and reticular veins in the lower extremities. Feb 01 2021
S4531 Iohexol Iohexol (Omnipaque) is a radiographic contrast agent that can be used as an exogenous filtration marker for accurate glomerular filtration rate (GFR) estimates. Feb 01 2021
S3375 Mitochondrial Fusion Promoter M1 Mitochondrial fusion promoter M1 is a mitochondrial dynamic modulator that increases the expression of mitofusin 2, a mitochondrial outer membrane fusion protein, reduces brain mitochondrial dysfunction. Mitochondrial fusion promoter M1 alleviates brain damage in rats with cardiac ischemia/reperfusion injury. Jan 26 2021
S0231 NSC15364 NSC 15364 (compound 59) is an inhibitor that directly interacts with VDAC1 and prevents VDAC1 oligomerization, concomitant with an inhibition of apoptosis. Jan 26 2021
S0503 Estrogen receptor modulator 1 Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM) with pIC50 of 0.46. Estrogen receptor modulator 1 exhibits potential anti-tumor activity. Jan 18 2021
S0275 DLin-KC2-DMA DLin-KC2-DMA is a useful lipid for lipid-based nanoparticle (LNP) delivery system. Jan 18 2021