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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC20626 ABT-089 ABT-089 (Pozanicline) is a potent, selective α4β2 nAChR agonist with Ki of 16 nM.
DC21984 ABT-100 ABT-100 (ABT100) is a highly selective, potent, orally bioavailable inhibitor of farnesyltransferase (FTase).
DC20628 ABT-102 ABT-102 is a potent, highly selective, orally active TRPV1 antagonist that inhibits agonist-evoked increases in intracellular Ca(2+) levels with IC50 of 5-7 nM.
DC20629 ABT-107 ABT-107 is a potent and selective α7 nAChR agonist with Ki of 0.2-0.6 nM for rat or human cortex α7 nAChRs.
DC2002 Venetoclax(ABT-199) Featured Venetoclax (ABT-199; GDC-0199) is a highly selective, orally bioavailable small-molecule inhibitor of Bcl-2, exhibiting sub-nanomolar binding affinity with a Ki of less than 0.01 nM. This compound has been demonstrated to induce autophagy, highlighting its role in modulating programmed cell death pathways. In vitro studies reveal that Venetoclax exhibits potent cytotoxic activity against FL5.12-BCL-2 cells, with an EC50 of 4 nM, while showing markedly reduced efficacy against FL5.12-BCL-XL cells (EC50 = 261 nM), underscoring its selectivity for Bcl-2 over Bcl-XL. The selectivity of Venetoclax is further corroborated in cellular mammalian two-hybrid assays, where it effectively disrupts BCL-2-BIM protein-protein interactions with an EC50 of 3 nM. In contrast, it demonstrates significantly weaker activity against BCL-XL-BCL-XS and MCL-1-NOXA complexes, with EC50 values of 2.2 μM, reinforcing its specificity for Bcl-2-dependent apoptotic regulation. In vivo efficacy studies utilizing xenograft models derived from RS4;11 cells, a representative model of acute lymphoblastic leukemia (ALL), demonstrate that a single oral dose of Venetoclax (12.5 mg/kg) achieves a maximal tumor growth inhibition (TGImax) of 47% (P < 0.001) and a tumor growth delay (TGD) of 26% (P < 0.05). These results indicate robust anti-tumor activity in a Bcl-2-dependent malignancy.
DC4127 ABT-263 (Navitoclax) Featured ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤ 1 nM, respectively.
DC23537 ABT-288 ABT-288 is a potent, selective and competitive antagonist of H3 receptor with Ki of 1.9/8.2 nM for human/rat H3 respectively.
DC7352 ABT-333 Featured ABT-333 is an NS5B non-nucleoside polymerase inhibitor.
DC10049 Tebanicline(ABT-594) Featured ABT-594 represents a novel class of broad-spectrum analgesics whose primary mechanism of action is activation of the neuronal nicotinic acetylcholine receptors.
DC9706 ABT-639 Featured ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker. ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50 = 2 μM) and attenuates LVA currents in rat DRG neurons (IC50 = 8 μM).
DC10723 ABT-702 Featured ABT-702 is a potent non-nucleoside adenosine kinase inhibitor (IC50 = 1.7 nM), selective over other sites of adenosine interaction (A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase).
DC9262 ABT-719 Featured ABT-719 is a potent bacterial DNA gyrase inhibitor.
DC9261 ABT-719 HCl Featured ABT-719 is a potent bacterial DNA gyrase inhibitor.
DC1022 ABT-737 Featured ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM, respectively.
DC7353 ABT-751(E 7010) Featured ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively.
DC4231 Linifanib (ABT-869) Featured ABT-869 is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of the vascular endothelial growth factor (VEGF) and platelet derived growth factor (PDGF) receptor families.
DC20630 ABTL0812 ABTL0812 is a novel first-in-class, small molecule that inhibits the Akt/mTORC1 axis and shows antiproliferative effect on tumor cells.
DC11155 ABX-1431 Featured ABX-1431 (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL).
DC11183 ABX-1431 hydrochloride Featured ABX-1431 (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL).
DC23182 ABX464 Featured ABX464 (ABX-464, ABX 464) is a novel class of anti-HIV small molecule targeting Rev-mediated viral RNA biogenesis, shows dose dependent inhibition of HIV-1 replication in stimulated PBMCs with IC50 of 0.1-0.5 uM.
DC7698 AC 55541 Featured AC 55541 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 6.7) that displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation.
DC11508 AC1903 Featured AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model.
DC10293 AC260584 AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
DC11149 AC261066 AC261066 (AC-261066, AC261) is a potent, selective, orally available RARβ2 agonist with pEC50 of 8.1, displays selectivity over RARβ1, RARα and RARγ (pEC50=6.4, 6.2 and 6.3).
DC12577 AC-263093 Featured AC-263093 (AC263093) is a potent, functionally selective neuropeptide FF receptor type 2 (NPFFR2) agonist with pKi of 6.9.
DC10117 AC264613 Featured AC264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5). Displays no activity at other PAR subtypes and exhibits no significant activity at over 30 other receptors implicated in nociception and inflammation.
DC20631 AC-265347 AC-265347 is a calcimimetic acting agent and highly efficacious, orally active allosteric agonist (PAM) of CaSR with IC50 of 10 nM in PI hydrolysis assays.
DC20300 AC-4-130 AC-4-130 is a novel, potent STAT5 SH2 domain inhibitor, binds to and efficiently blocks STAT5 activation and subsequent transcriptional activity, shows high selectivity for STAT5 over STAT1 and STAT3.
DC21863 AC5 inhibitor C90 AC5 inhibitor C90 is a novel potent, selective adenylyl cyclase type 5 (AC5) inhibitor with IC50 of 30 nM, >5-fold selectivity over AC2 and AC6 subtypes.
DC12086 AC-55649 Featured AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
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