IAP|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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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.

References:

1.Fulda S. Int Rev Cell Mol Biol. 2017;330:157-169.

2.Silke J,et al. Methods Enzymol. 2014;545:35-65.

Cat. No.	Product Name	CAS No.	Information
H6281	Xevinapant	1071992-99-8	DEBIO 1143 (AT-406, DEBIO-1143, SM406, ARRY-334543, D1143) is potent, orally active Smac mimetic that antagonizes cIAP1, cIAP2 and XIAP with Ki of 66.4, 1.9 and 5.1 nM, respectively; effectively antagonizes XIAP BIR3 protein in cell-free functional assays, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines; effectively induces apoptosis and causes complete inhibition of tumor growth apoptosis in xenograft tumors.
H1655	YM-155 hydrochloride	355406-09-6	A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM; does not significantly inhibit SV40 promoter activity (>30 uM); suppresses expression of survivin and induces apoptosis in PC-3 and PPC-1 human HRPC cell lines at 10 nM, without effect on IAP- or Bcl-2-related proteins; induces massive tumor regression in PC-3 tumor mice model (3-10 mg/kg).
H1654	YM-155	781661-94-7	A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM; does not significantly inhibit SV40 promoter activity (>30 uM); suppresses expression of survivin and induces apoptosis in PC-3 and PPC-1 human HRPC cell lines at 10 nM, without effect on IAP- or Bcl-2-related proteins; induces massive tumor regression in PC-3 tumor mice model (3-10 mg/kg).
H1653	UC-112	383392-66-3	UC-112 is a novel IAP inhibitor that potently inhibits human melanoma (A375 and M14) and human prostate (PC-3 and DU145) cancer cell lines with IC50 of 0.7-3.4 uM; also potently inhibits the growth of P-gp-overexpressed multidrug-resistant cancer cells, strongly activates caspase-3/7 and caspase-9 activities, and selectively downregulates survivin level at 1 uM; strongly inhibits tumor growth and reduces both X chromosome-linked IAP and survivin levels in an A375 human melanoma xenograft model in vivo.
H1652	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.
H1651	SM-1295	1562375-46-5	SM-1295 is a potent, selective cIAP1 and cIAP2 inhibitor with Ki of 900-fold for cIAP1 over XIAP; potently inhibits cell growth in the MDA-MB-231 and SK-OV-3 cancer cell lines and induces apoptosis at low nanomolar concentrations; efficiently induces degradation of cIAP1 protein in cancer cells, as well as cleavage of PARP, caspase-8, and caspase-3; induces cell death in a TNFα-dependent manner in both MDA-MB-231 and SK-OV-3 cancer cell lines.
H1650	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.
H1649	MX107	2170102-50-6	MX107 is a novel potent survivin inhibitor, effectively suppresses MDA-MB-231 cells proliferation with IC50 of 3.1 uM; significantly enhances the tumoricidal efficacy of doxorubicin in TNBC cells, induces degradation of XIAP and/or cIAP1, which inhibited NF-κB activation by genotoxic agents.
H1648	MX106	2170836-81-2	MX106 is a novel potent survivin inhibitor, effectively suppresses MDA-MB-231 cells proliferation with IC50 of 2.2 uM; significantly enhances the tumoricidal efficacy of doxorubicin in TNBC cells, induces degradation of XIAP and/or cIAP1, which inhibited NF-κB activation by genotoxic agents.
H1647	MV1	1001600-54-9	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.

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