IAP Antagonist

Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with K_ds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.

BV6 is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family. BV6 shows an IC₅₀ of 7.2 μM in MTS assays in HCC193 cells. BV6 can be used in the research of endometrial cancer and endometriosis.

Tolinapant (ASTX660) is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).

Dasminapant (APG-1387), a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). Dasminapant induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. Dasminapant can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma.

SM-1295 is an inhibitor of apoptosis protein (IAP) antagonist, with K_d values of 3077 nM, 3.2 nM and 9.5 nM for XIAP-BIR3, c-IAP1-BIR3 and c-IAP2-BIR3, respectively.

MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand.

CST530 is an inhibitor of apoptosis protein (IAP) antagonist. CST530 is an IAP-type Ligands for E3 Ligase. CST530 binds to the BIR3 domain of IAP and interferes with its function, thereby promoting the ubiquitination and degradation of cIAP1. CST530 can be used to prepare PROTACs.

BV6 TFA is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family. BV6 TFA shows an IC₅₀ of 7.2 μM in MTS assays in HCC193 cells. BV6 TFA can be used in the research of endometrial cancer and endometriosis.

Embelin (Standard) is the analytical standard of Embelin. This product is intended for research and analytical applications. Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells.

GDC-0152-acetamide is a pan-inhibitor of apoptosis protein (IAP) antagonist. GDC-0152-acetamide induces cIAP1/2 autoubiquitination and degradation, activating the non-canonical NF-κB pathway to promote TNF-α secretion and tumor cell apoptosis. GDC-0152-acetamide is promising for research of ERα-positive breast cancer.

β-carotene-15,15ʹ-epoxide is a XIAP antagonist with apoptosis-inducing and antitumor activity, found in the leaves of Spondias mombin. In a DMBA (HY-W011845)-induced rat model of breast cancer, β-carotene-15,15ʹ-epoxide binds to the BIR3 domain of the anti-apoptotic protein XIAP, blocking its interaction with caspase-9 and thereby promoting tumor cell apoptosis. In addition, β-carotene-15,15ʹ-epoxide significantly downregulates the expression of BCL-2, COX-2, and TNF-α in tumor tissues, reduces MDA levels, increases catalase activity, and modulates serum levels of LDH, ALP, and ALT, demonstrating strong antioxidant, anti-inflammatory, and metabolic protective effects. β-carotene-15,15ʹ-epoxide may be used in research on inflammation-related conditions and cancers such as breast cancer.