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You are here:Home-Inhibitors & Agonists-Apoptosis-IAP

Request The Product List ofIAP IAP

    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.

Cat. No. Product Name CAS No. Information
GY02836

ASTX660

1799328-86-1

ASTX660 is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM; potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cell; induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts.

GY05381

MV1

1001600-54-9

MV 1 is 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; induces cell death that is dependent on TNF signaling and de novo protein biosynthesis.

GY02318

AZD5582

1258392-53-8

AZD5582 is a dimeric Smac mimetic, potent IAP antagonist that binds potently to the BIR3 domains of cIAP1, cIAP2 and XIAP with IC50 of 15, 21and 15 nM, respectively; causes cIAP1 degradation and induces apoptosis in the MDA-MB-231 breast cancer cell line at subnanomolar concentrations in vitro; induces cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions in MDA-MB-231 xenograft-bearing mice.

GY02054

BV6

1001600-56-1

A small molecule, bivalent IAP antagonist that binds to the c-IAP1 and XIAP BIR2-BIR3 domains with Kd of 0.46 and 0.029 nM, respectively; results in dramatic induction of auto-ubiquitination activity and rapid proteasomal degradation of c-IAPs; also induces induce TNFα-dependent cell death, exhibits single-agent cell killing activity in EVSA-T cell line (IC50=14 nM).

GY05232

ASTX660 hydrochloride

1799328-50-9

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; potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cell; induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts.

GY05231

ASTX660 mesylate

1799328-90-7

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; potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cell; induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts.

GY05341

CS3

1207457-11-1

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).

GY05340

PS1

1207994-72-6

PS1 is a potent inhibitor of IAP family with IC50 of 36/96/33 nM for c-IAP1/c-IAP2/XIAP respectively.

GY05319

T-3256336

1266227-69-3

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; dose dependently antagonizes XIAP and promotes the activities of caspase-3 with EC50 of 1.3 uM in cell-free assays, induces the rapid proteasomal degradation of cIAP-1 and activates TNF-α-dependent extrinsic apoptosis signaling in cultured cells; induces cIAP-1 degradation, TNF-α production and caspase activation in cancer xenograft models.

GY05293

AT-IAP

1403898-55-4

A potent, orally bioavailable, dual XIAP/cIAP1 inhibitor with EC50 of 5.1/0.32 nM, respectively; exhibits MDA-MB-231 cell proliferation inhibition with IC50 of 4.4 nM; decreases basal and TNF-α-induced cIAP-1 expression in CaP cells, switches TNF-α signaling from pro-survival to pro-apoptotic and increases radiation sensitivity of CaP cells in co-culture with THP-1 cells; shows in vivo efficacy in Balb/c scid mice bearing MDA-MB-231 xenografts.

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