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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC24065 EPZ-011989 trifluoroacetate A potent, selective, orally bioavailable inhibitor of EZH2 with Ki of < 3 nM.
DC23552 AS-2444697 HCl Featured A potent, selective, orally bioavailable IRAK-4 inhibitor that potently inhibits human and rat IRAK-4 activity with subnanomolar order, >30-fold selectivity over IRAK-1.
DC11835 AM-8553 A potent, selective, orally bioavailable MDM2-p53 interaction inhibitor with HTRF IC50 of 1.1 nM, SJSA-1 EdU IC50 of 68 nM.
DC11677 CCT-271850 A potent, selective, orally bioavailable Mps1 kinase inhibitor with IC50 of 11 nM.
DC22941 AZD-9056 A potent, selective, orally bioavailable P2X7 receptor antagonist.
DC11841 LAS191954 A potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 of 2.6 nM.
DC21607 SB-649868 Featured SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).
DC21598 RWJ-56110 A potent, selective, peptide-mimetic PAR-1 antagonist with binding IC50 of 0.44 uM, with no effect on PAR-2, PAR-3, or PAR-4.
DC20691 ASP 3652 A potent, selective, peripherally active and orally available FAAH inhibitor for treatment of chronic prostatitis/chronic pelvic pain syndrome..
DC11748 LY2033298 Featured LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms.
DC23043 Tpl2-IN-2p A potent, selective, reversible and ATP-competitive inhibitor of Tpl2 kinase with IC50 of 50 nM.
DC23933 MK-0893 A potent, selective, reversible and competitive antagonist of glucagon receptor with high binding affinity (IC(=50=6.6 nM) and functional cAMP activity (IC50=15.7 nM).
DC11691 NSC95397 Featured A potent, selective, reversible Cdc25 dual specificity phosphatase inhibitor with Ki of 32/96/40 nM for Cdc25A/B/C, respectively.
DC11978 SB 265610 Featured SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist.
DC20412 II-B08 A potent, selective, reversible inhibitor of PTP SHP2 with IC50 of 5.5 uM, exhibits >3-fold selectivity for SHP2 over other PTPs.
DC11875 GlpG inhibitor 11 A potent, selective, reversible rhomboid proteases inhibitor with Ki of 45 nM for GlpG .
DC11713 NSC-109555 ditosylate A potent, selective, reversible, ATP-competitive Chk2 inhibitor with IC50 of 0.2 uM.
DC11724 MS-453 A potent, selective. covalent protein lysine methyltransferase SETD8 inhibitor with IC50 of 804 nM.
DC22892 KNT-127 A potent, selectove δ-opioid receptor agonist with Ki of 0.16 nM, dispalys 133.5-fold and 960.5-fold selectivity over μOR and κOR respectively.
DC22563 TN1 A potent, small molecule fetal hemoglobin (HbF) inducer with EC50 of 100 nM.
DC20606 8-Thioquinoline A potent, small molecule inhibitor of the proteasome subunit Rpn11 with IC50 of 2.5 uM..
DC11951 Bischof-5 A potent, specfic casein kinase 1δ (CK1δ) inhibitor with IC50 of 40 nM.
DC11983 CX797 A potent, specfic CXCR2 antagonist that inhibits IL8 down-regulation of forskolin-induced cAMP with IC50 of 7.79 uM.
DC21321 ML349 Featured A potent, specific acyl protein thioesterase 2 (APT-2, LYPLA2) inhibitor with IC50 of 144 nM and Ki of 120 nM, >20-fold selectivity over APT-1 and serine hydrolase enzyme family.
DC22529 FPTQ A potent, specific and allosteric mGluR1 antagonist with IC50 of 6 nM and 1.4 nM for human and mouse mGluR1, respectively..
DC25075 Sivelestat sodium A potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM.
DC23074 Sivelestat Featured A potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM.
DC23494 GRI 977143 Featured A potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM).
DC24105 MK-0591(Quiflapon ) Featured A potent, specific and orally active 5-Lipoxygenase-activating protein (FLAP) inhibitor with IC50 of 1.6 nM in FLAP binding assay.
DC11556 trans-AUCB A potent, specific and orally bioavailable soluble epoxide hydrolase (sEH) inhibitor with IC50 of 1.3 nM.

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