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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC20686 AS602868 A potent, selective and ATP-competitive inhibitor of IKK2 with IC50 of 60 nM and Ki of 20 nM, also interfers directly with FLT3 kinase activation.
DC22817 RUSKI-201 A potent, selective and cell active Hedgehog acyltransferase (Hhat) inhibitor with IC50 of 0.87 uM.
DC11820 A-893 A potent, selective and cell active lysine methyltransferase SMYD2 inhibitor with IC50 of 2.8 nM.
DC22867 HR22C16 A potent, selective and cell permeable inhibitor of mitotic kinesin Eg5 with IC50 of 0.8 uM, does not interact with other microtubule motor proteins.
DC20309 ANTISAUVAGINE-30 Featured A potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist with Ki of 1.4 nM, 100-fold selectiivity over CRF1.
DC11979 SB 332235 A potent, selective and competitive CXCR2 inhibitor that selectively inhibits CXCR2-mediated recruitment of β-arrestin-2 with pKi of 8.92.
DC11755 L-732138 Featured A potent, selective and competitive NK1 receptor antagonist with IC50 of 2.3 nM.
DC22763 Rilapladib A potent, selective and oral lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.23 nM, for the treatment of Alzheimer's disease and atherosclerosis..
DC21210 Rolofylline A potent, selective and orally active adenosine A1 receptor antagonist with Ki of 1.3 nM.
DC21827 XE 991 dihydrochloride Featured A potent, selective and orally active blocker of voltage-gated potassium channels Kv7 (KCNQ) that blocks KCNQ1, KCNQ2 and KCNQ2+KCNQ3 with Kd of 0.78, 0.7 and 0.6 uM, respectively.
DC23371 NI-42 Featured NI-42 is a potent, selective and orally active BRPF1 bromodomain inhibitor with IC50 of 7.9 nM, with excellent selectivity over nonclass IV BRDs; weakly inhibits BRPF2 (BRD1), BRPF3, BRD9 and BRD4 (BD1) with IC50 of 48, 260, 310 and 4500 nM respectively, and no activity for ATAD2A/2B (IC50>100 uM); shows a modest (GI50=1-10 uM) and selective inhibition of proliferation of certain cancer lines, particularly those lines exhibiting monocytic lineage differentiation; a novel, structurally orthogonal chemical probe for the BRPFs suitable for cellular and in vivo studies.
DC11710 GDC-0425 A potent, selective and orally active Chk1 inhibitor.
DC24158 Rofecoxib A potent, selective and orally active COX-2 inhibitor with IC50 of 26 nM for inhibition of the COX-2-dependent production of PGE2 in human osteosarcoma cells.
DC20810 Pexacerfont A potent, selective and orally active CRF1 receptor antagonist with IC50 of 6.1 nM, >1,000-fold selectivity over CRF-binding protein and biogenic amine receptors.
DC20923 CP 376395 hydrochloride A potent, selective and orally active CRF1 receptor antagonist with Ki of 12 nM, shows no affinity for CRF2 receptor (Ki>10 uM).
DC20689 ASB 14780 A potent, selective and orally active cytosolic phospholipase A2α (cPLA2α) inhibitor with IC50 of 20 nM.
DC11868 Freselestat A potent, selective and orally active human neutrophil elastase (HNE) inhibitor with Ki of 12 nM.
DC21689 SR 142948A Featured A potent, selective and orally active neurotensin receptor antagonist with IC50 of 1.19 nM.
DC23621 YM543 A potent, selective and orally active SGLT2 inhibitor with IC50 of 8.9 nM, 280-fold selectivity over SGLT1.
DC11514 Atogepant A potent, selective and orally available CGRP receptor antagonist for the prevention of migraine. Migraine.
DC21842 Darexaban A potent, selective and orally available factor Xa (FXa) inhibitor with IC50 of 54.6 nM.
DC21718 T-3364366 A potent, selective and orally available inhibitor of delta-5 desaturase (D5D) with Ki of <2.7 nM and IC50 of 19 nM, with excellent selectivity over D6D and SCD.
DC20768 Tonapofylline A potent, selective and orally bioavailable adenosine A1 (A1A) receptor antagonist with Ki of 7 nM.
DC22682 INCB9471 A potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs.
DC23643 JNJ 54166060 A potent, selective and orally bioavailable P2X7 receptor with IC50 of 4 nM and 115 nM for hP2X7 and rP2X7, respectively.
DC21600 S1P Lyase inhibitor 31 A potent, selective and orally bioavailable S1P lyase (S1PL) inhibitor with enzyme IC50 of 44 nM, cell IC50 of 110 nM.
DC23207 JNJ-17203212 Featured A potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively.
DC21464 Eribaxaban A potent, selective and orally efficacious factor Xa (FXa) inhibitor with IC50 of 0.32 nM.
DC25047 Calphostin C A potent, selective and photo-dependent inhibitor of PKC with IC50 of 50 nM.
DC11511 A-485 Featured A potent, selective and, cell and in vivo active p300/CBP catalytic inhibitor with IC50 of 9.8/2.6 nM.
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