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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M10811 | CUDC-427 | CUDC-427 (GDC-0917) is a highly effective IAP inhibitor commonly used in research on a variety of cancers. |
| M10782 | APG-1387 | APG-1387 is a divalent SMAC mimetic that is an IAP antagonist that blocks the activity of the IAP family of proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). APG-1387 induces degradation of cIAP-1 and XIAP proteins as well as caspase-3 activation and PARP lysis, leading to apoptosis. APG-1387 can be used for the study of hepatocellular carcinoma, ovarian cancer and nasopharyngeal carcinoma. |
| M10702 | AZD5582 | AZD5582 is an IAP antagonist that can be effectively combined with bir3 domains of cIAP1, cIAP2, and XIAP, IC50 The values are 15, 21, 15 nM, respectively. AZD5582 Induces apoptosis. |
| M9933 | Tolinapant(ASTX660) | ASTX660 is a potent, non-peptidomimetic antagonist of cIAP1/2 and XIAP, it potently inhibited the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively. |
| M6187 | SM-164 | SM-164 is a potent cell-permeable and bivalent Smac mimetic which bind to a XIAP protein with a Ki value of 0.56 nM, and binds to cIAP-1 and cIAP-2 proteins with Ki values of 0.31 and 1.1 nM, respectively. |
| M5611 | Embelin | Embelin is a cell-permeable benzoquinone compound that exhibits antitumor properties. Specifically antagonizes XIAP-mediated inhibition of caspase-9 activation by directly targeting the Smac and caspase-9 binding domain BIR3 (IC50 = 4.1 uM in a competitive binding assay with Smac peptide). |
| M4801 | LCL161 | LCL161 is an orally bioavailable SMAC mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP). |
| M3638 | BV6 | BV6 is a small-molecule Smac mimetic, which antagonizes IAP proteins. |
| M2166 | Birinapant | Birinapant (TL32711) is a bivalent Smac analogue, which is a potent antagonist of XIAP and cIAP1 with Kd values of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces autoubiquitination and proteasome degradation of cIAP1 and cIAP2 in intact cells, resulting in the formation of RIPK1: Caspase-8 complex, which activates and induces tumor cell death. |
| M2138 | GDC-0152 | GDC-0152 is a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins with potential antineoplastic activity. |
| M2026 | AT-406 | AT-406 is an orally bioavailable potent IAP (inhibitor of apoptosis protein) of XIAP, cIAP1 and cIAP2 with Ki of 66.4 nM, 1.9 nM and 5.1 nM, respectively. |
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