IAP (Inhibitors of Apoptosis) is a family of functionally and structurally related proteins, which serve as endogenous inhibitors of programmed cell death (apoptosis). A common feature of all IAPs is the presence of a BIR in one to three copies. The human IAP family consists of 8 members, and IAP homologs have been identified in numerous organisms. The members of the IAPs included IAPs, Cp-IAP, Op-IAP, XIAP, c-IAPl, C-IAP2, NAIP, Livin and Survivin. The best characterized IAP is XIAP, which binds caspase-9, caspase-3 and caspase 7, thereby inhibiting their activation and preventing apoptosis. Also cIAP1 and cIAP2 have been shown to bind caspases, although how the IAPs inhibit apoptosis mechanistically at the molecular level is not completely understood.
||Birinapant a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kd values of 45 nM and < 1 nM, respectively.
||LCL161 is a novel IAP inhibitor, inhibits XIAP activity in HEK293 cell with IC50 of 35 nM, also inhibits cIAP1 activity in MDA-MB-231 cell with IC50 of 0.4 nM.
||AT406 (SM-406) is a potent Smac mimetic and an antagonist of IAP (inhibitor of apoptosis protein via E3 ubiquitin ligase), binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide. Phase 1.
||GDC-0152 is a potent inhibitor of IAPs which binds to the XIAP BIR3 domain, the BIR domain of ML-IAP, and the BIR3 domains of cIAP1 and cIAP2 with Ki values of 28, 14, 17, and 43 nM, respectively.
||Embelin (Embelic acid)
||Embelin is a cell-permeable benzoquinone compound that exhibits antitumor properties.
||BV6 is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.
||AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively).
||ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
||SM-164 is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.
||MX106 is a novel potent survivin inhibitor, effectively suppresses MDA-MB-231 cells proliferation with IC50 of 2.2 uM.
||MX107 is a novel potent survivin inhibitor, effectively suppresses MDA-MB-231 cells proliferation with IC50 of 3.1 uM.
||ASTX660 mesylate is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM.
||ASTX660 hydrochloride is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM.
||SM-1295 is a potent, selective cIAP1 and cIAP2 inhibitor with Ki of <10 nM, displays >900-fold for cIAP1 over XIAP.
||A potent, orally bioavailable, dual XIAP/cIAP1 inhibitor with EC50 of 5.1/0.32 nM, respectively.
||A potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively.
||PS1 is a potent inhibitor of IAP family with IC50 of 36/96/33 nM for c-IAP1/c-IAP2/XIAP respectively..
||CS3 is a potent, selective cIAP1 and cIAP2 inhibitor with IC50 of 16 nM and 85 nM respectively, shows no significant activity against XIAP (IC50>34 uM)..
||A small-molecule IAP antagonist that binds to select baculovirus IAP repeat (BIR) domains resulting in dramatic induction of auto-ubiquitination activity and rapid proteasomal degradation of c-IAPs.