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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC22696 BRL 44408 Featured A potent, selective α2A-adrenoceptor antagonist with Ki of 1.7 nM, 80-fold selectivity over α2B-adrenergic receptors.
DC22695 BRL 44408 maleate A potent, selective α2A-adrenoceptor antagonist with Ki of 1.7 nM, 80-fold selectivity over α2B-adrenergic receptors.
DC22694 ARC 239 dihydrochloride A potent, selective α2B adrenoceptor antagonist with pKd of 8.8, 200-fold selectivity over α2A, and α2D receptors.
DC22753 NS13001 Featured NS13001 is a highly selective and orally bioavailable allosteric positive modulator targeting small-conductance calcium-activated potassium (SK) channels. It exhibits potent activity, with EC50 values of 1.8 μM for SK2 and 0.14 μM for SK3, demonstrating greater potency toward SK3. Due to its pharmacological profile, NS13001 has emerged as a promising candidate for treating spinocerebellar ataxia type 2 (SCA2) and may also have therapeutic potential in other forms of cerebellar ataxia.
DC11745 BMS-22 A potent, selective, allosteric CCR2 antagonist with binding IC50 of 5.1 nM.
DC11744 CCR2-RA-[R] A potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM..
DC21316 ML400 A potent, selective, allosteric LMPTP inhibitor with IC50 of 1.68 uM, displays good selective against other phosphatases.
DC22916 JNJ-10397049 A potent, selective, and bioavailable OX2 receptor antagonist with Kb of 4.5 nM.
DC23971 LY450108 A potent, selective, and centrally active positive allosteric modulator of AMPAR-mediated neurotransmission, which increase ion channel flux in the presence of agonist by suppressing desensitization and/or deactivation of the receptors..
DC24030 LY451395 Featured A potent, selective, and centrally active positive allosteric modulator of AMPAR-mediated neurotransmission, which increase ion channel flux in the presence of agonist by suppressing desensitization and/or deactivation of the receptors..
DC23963 QL-47 A potent, selective, and irreversible BTK inhibitor with IC50 of 7 nM.
DC21545 PXS-4681A A potent, selective, and irreversible inhibitor of SSAO/VAP-1 (AOC3) with Ki of 37 nM, IC50 of <10 nM.
DC11850 MK-7145 A potent, selective, and oral renal outer medullary potassium channel (ROMK) inhibitor with IC50 of 68 nM.
DC11727 RO-2468 A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 6 nM.
DC11728 RO-5353 A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 7 nM.
DC21254 LY-517717 A potent, selective, and orally bioavailable factor Xa (FXa) inhibitor for prevention and treatment of thromboembolic diseases..
DC21487 PF-05190457 Featured A potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36.
DC23541 IRAK4-IN-16 A potent, selective, and orally bioavailable inhibitor of interleukin-1 receptor-associate kinase-4 (IRAK4) with IC50 of 2.8 nM, 217- and 892-fold selectivity over IRAK-1 and TAK1, respectively.
DC23949 CX-6258 hydrochloride hydrate A potent, selective, and orally efficacious pan-Pim inhibitor with IC50 of 5/25/16 nM for Pim1/2/3, respectively.
DC23036 BI-69A11 A potent, selective, ATP competitive AKT inhibitor with IC50 of 2.3 uM for Akt1.
DC22651 PF-4950834 A potent, selective, ATP-competitive and orally acitve Rho kinase inhibitor with IC50 of 33.1 and 8.5 nM for ROCK1 and ROCK2, respectively.
DC23867 PF-00337210 A potent, selective, ATP-competitive and orally bioavailable inhibitor of VEGFR-2 with Ki of 0.7 and 8.8 nM for unactivated and fully phosphorylated VEGFR-2, respectively.
DC11711 VER-158411 A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.
DC11733 SAR-020106 A potent, selective, ATP-competitive Chk1 inhibitor with IC50 of 13.3 nM.
DC12007 SOMG-833 A potent, selective, ATP-competitive c-MET inhibitor with IC50 of 0.93 nM.
DC23930 Bay 65-1942 A potent, selective, ATP-competitive inhibitor of IKKβ kinase with Ki of 2 nM.
DC22500 Bay 65-1942 hydrochloride A potent, selective, ATP-competitive inhibitor of IKKβ kinase with Ki of 2 nM.
DC23070 MAP4K4-IN-11e A potent, selective, ATP-competitive inhibitor of MAP4K4 with IC50 of 1.9 uM, without effect on other stress pathway related kinases.
DC23964 BMS-509744 A potent, selective, ATP-competitive ITK inhibitor with IC50 of 19 nM.
DC22551 DFMTI A potent, selective, brain penetrant and orally active mGluR1 antagonist with 4.3 nM and 3.6 nM for huam and rat mGluR1, respectively.

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