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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC23635 YM 758 A novel potent "funny" If current channel (If channel) inhibitor that inhibits rOct1- and hOCT1-mediated [3H]MPP uptake with IC50 of 23.8 and 40.5 uM, respectively.
DC23542 LY3031207 A novel potent (IC50=910 ng/mL), highly selective microsomal prostaglandin E synthase 1 inhibitor (mPGES-1) for treatment of undisclosed indications..
DC11994 ZQ-16 A novel potent and selective agonist of GPR84 that induces calcium response with EC50 of 0.213 uM.
DC23841 EW-7195 Featured A novel potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 4.83 nM, dispalys >300-fold selectivity over p38α.
DC22734 UR-1102 A novel potent and selective, orally active URAT1 inhibitor with Ki of 57 nM, 130 and 42-fold selectivity over OAT1 and OAT3, respectively.
DC20826 BPR1K653 hydrochloride A novel potent Aurora kinase inhibitor that inhibits Aurora-A and Aurora-B with IC50 of 24 nM and 45 nM, respectively.
DC21048 GIV3727 A novel potent bitter receptor (TAS2Rs) antagonist that inhibits activation of hTAS2R31 by saccharin and acesulfame K with IC50 of 6.4 and 7.9 uM respectively.
DC20534 Revosimeline A novel potent cannabinoid receptor agonist..
DC20435 Leucettine L41 A novel potent cdc2-like kinase (CLKs) and DYRKs inhibitor with IC50 of 40, 35 and 15 nM for DYRK1A, DYRK2 and CLK1, respectively.
DC21453 Riviciclib A novel potent CDK inhibitor with IC50 of 79 nM, 63 nM and 20 nM for Cdk4/cyclin D1, Cdk1/cyclin B and Cdk9/cyclin T1, respectively.
DC22743 OSSK-674842 A novel potent CFTR potentiator that blocks hCFTR with apparent Kd of 71.3 uM.
DC22739 OSSK-630513 A novel potent CFTR potentiator with Kd of 31.7 nM.
DC21855 ZINC 39395747 Featured ZINC 39395747 is a novel potent derivative of propylthiouracil that functions as a cell-active inhibitor of cytochrome b5 reductase 3 (CYB5R3) with IC50 of 9.14 uM.
DC11600 D211 A novel potent DNA-intercalating payload dimer (PBD dimer) payload for antibody-drug conjugates (ADCs).
DC20437 Linzagolix A novel potent gonadotrophin releasing hormone (GnRH) antagonist..
DC20482 Opigolix A novel potent gonadotrophin releasing hormone (GnRH) antagonist..
DC22861 CRT-0105950 A novel potent LIMK inhibitor with IC50 of 0.3 nM and 1 nM for LIMK1 and LIMK2, respectively.
DC22862 CRT-0105446 A novel potent LIMK inhibitor with IC50 of 8 nM and 32 nM for LIMK1 and LIMK2, respectively.
DC11622 MAP3K14-IN-173 A novel potent MAP3K14 kinase inhibitor with IC50 of 1.8 nM (NIK autophosphorylation).
DC11515 Azeloprazole A novel potent proton pump inhibitor that irreversibly inhibits H+,K+-ATPase activity with IC50 of 0.28 uM.
DC23393 BETi-211 A novel potent small-molecule BET bromodomain (BRD) inhibitor that binds to BET proteins with Ki values of <1 nM.
DC11995 BI 703704 A novel potent soluble guanylate cyclase (sGC) activator.
DC11880 TH1834 A novel potent specific histone acetyltransferaseTip60 inhibitor.
DC11881 TH1834 dihydrochloride A novel potent specific histone acetyltransferaseTip60 inhibitor.
DC22798 ADA-07 A novel potent TOPK inhibitor that effectively suppresses SUV-induced activation of MAPKs signal transduction resulting in reduced SUV-induced skin carcinogenesis.
DC11603 SR-19871 A novel potent ULK1 inhibitor with IC50 of 11 nM..
DC11693 AJS1669 sodium A novel potent, allosteric, orally available muscle glycogen synthase 1 (GYS1) activator with EC50 of 5.2 uM.
DC11692 AJS1669 A novel potent, allosteric, orally available muscle glycogen synthase 1 (GYS1) activator with EC50 of 5.2 uM.
DC21354 MT47-100 Featured MT47-100 is a novel compound that exhibits a unique dual functionality as both an allosteric activator and inhibitor of AMP-activated protein kinase (AMPK) complexes, depending on the isoform present. Specifically, MT47-100 acts as a direct activator of AMPK complexes containing the β1 isoform and as a direct inhibitor of AMPK complexes containing the β2 isoform. This isoform-specific modulation of AMPK activity makes MT47-100 a potentially valuable tool for studying the distinct physiological roles of β1- and β2-containing AMPK complexes, as well as a candidate for therapeutic applications targeting AMPK-related pathways.
DC23525 AAT-008 A novel potent, and selective prostaglandin EP4 receptor antagonist with binding IC50 of 2.4 nM.

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