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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC22688 AZD 3676 A novel potent, combined serotonin 5-HT1A and 5-HT1B receptor antagonist with Ki of 0.13 and 2.4 nM in brain homogenates, respectively.
DC11986 OX03050 A novel potent, competitive squalene synthase inhibitor that upregulate the LDLR in mouse and human liver cell lines with EC50 of 26 nM.
DC20692 ASP 8477 A novel potent, highly selective fatty acid amide hydrolase (FAAH) inhibitor with IC50 of 0.99, 1.65 and 57.3 nM for human FAAH-1, FAAH-1 (P129T) and FAAH-2, respectively.
DC21507 PHA-408 A novel potent, highly selective, ATP-competitive IKK-2 inhibitor with IC50 of 40 nM, 350-fold selectivity over IKK-1.
DC23309 BCL6 inhibitor 8c A novel potent, in vivo-active BCL6 inhibitor with IC50 of 0.1 uM in ELISA assays.
DC21209 KW-2581 A novel potent, irreversible and orally active inhibitor of steroid sulfatase (STS) with IC50 of 13 nM in ZR-75-1 cells.
DC11769 MPO-IN-28 Featured A novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM.
DC21058 GNS-1481 A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 6.2, 3.4 and 4.2 nM for L858R-T790M, T790M and Del19-T790M, respectively.
DC21059 GNS-1486 A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 8.3, 4.2 and 4.3 nM for L858R-T790M, T790M and Del19-T790M, respectively.
DC11612 KBP-7018 hydrochloride A novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively.
DC11611 KBP-7018 A novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively.
DC11751 UHC1 A novel potent, non-agonist PPARγ ligand that blocks CDK5-mediated PPARγ phosphorylation, without the classical agonism.
DC11750 SR-1664 Featured SR-1664 is a novel potent, non-agonist PPARγ ligand that blocks the Cdk5-mediated phosphorylation in vitro (IC50=80 nM) and in vivo, without the classical agonism.
DC11968 OSU-03013 A novel potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) with IC50 of 2 uM.
DC24024 Z-360 A novel potent, orally active CCK-2/gastrin receptor antagonist with Ki of 0.47 nM.
DC11607 JTZ-951(Enarodustat) Featured A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2.
DC11608 JTZ-951 hydrochloride A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2.
DC11546 Azeloprazole sodium A novel potent, orally active proton pump inhibitor that irreversibly inhibits H+,K+-ATPase activity with IC50 of 0.28 uM.
DC21707 STX-681 A novel potent, orally active, dual-acting aromatase and steroid sulfatase (STS) inhibitor with ICI0 of 0.82 nM and 39 nM, respectively.
DC11599 PF-739 A novel potent, pan-AMPK activator with similar potency for all AMPK heterotrimers.
DC20806 BMS-852927 A novel potent, partial LXRβ-selective agonist (EC50=9 nM) with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays.
DC11610 AKS1-IN-19 A novel potent, selective and orally active ASK1 (MAP3K5) inhibitor with pIC50 of 8.3.
DC22745 SLx-4090 Featured A novel potent, selective and orally active enterocytic microsomal triglyceride transfer protein (MTP) inhibitor that inhibits only MTP localized to enterocytes with IC50 of 6 nM.
DC11696 CM-579 A novel potent, selective and reversible dual inhibitor of G9a/DNMTs with IC50 of 16 nM and 32 nM for G9a and DNMT1, respectively.
DC21667 SMM-295 A novel potent, selective cannabinoid receptor 2 (CB2) agonist with Ki of 12 nM, >30-fold selectivity over CB1.
DC20841 BRD6989 Featured A novel potent, selective CDK8 inhibitor with IC50 of 0.5 uM against recombinant Cyclin C/CDK8 complex.
DC11953 MU 380 A novel potent, selective CHK1 inhibitor 2 nM, >80-fold selectivity over CHK2.
DC11982 CX815 A novel potent, selective CXCR2 inhibitor with IC50 of 0.4 nM.
DC11981 CX4152 A novel potent, selective CXCR2 inhibitor with IC50 of 7.6 nM.
DC11827 9-ING-41 Featured 9-ING-41 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor[1]. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK-3β. 9-ING-41 has anticancer activity[2].

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