cIAP-2 Antagonist

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.

AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC₅₀s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.

Xevinapant (AT-406) is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with K_i of 66.4, 1.9, and 5.1 nM, respectively.

SM-164 hydrochloride 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.

HM90822 is an orally active IAP antagonist. HM90822 induces ubiquitination and proteasome-dependent degradation of XIAP, cIAP1 and cIAP2 in sensitive pancreatic cancer cells. HM90822 induces Apoptotic cell death. HM90822 inhibits tumor growth in Panc-1 pancreatic cancer xenograft and orthotopic mouse models. HM90822 can be used for the research of pancreatic cancer.

GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer.

Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with K_is of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors.

AZD5582 dihydrochloride is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC₅₀s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.

KHS108-MV1 is a conjugate of KHS108 and MV1. KHS108 is a ligand for TACC3. MV1 is an IAP antagonist that binds to cIAP1, cIAP2, and XIAP. KHS108-MV1 can be used in the research of breast cancer and fibrosarcoma.