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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.
| Molecular Weight | 1157.4 |
| Formula | C60H72N10O10S2 |
| CAS Number | 1570231-89-8 |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related IAP Products |
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Xevinapant (Debio1143,AT-406, SM-406) is a potentially first-in-class, highly potent oral antagonist of inhibitor of apoptosis protein (IAP), which not only promotes cancer cell death by inhibiting IAP, but also It can enhance the anti-tumor immune response by inhibiting IAP. |
| GDC-0152
GDC-0152 is a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins with potential antineoplastic activity. |
| 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. |
| BV6
BV6 is a small molecule Smac analog that antagonizes cIAP1 and XIAP. |
| LCL161
LCL161 is an orally bioavailable SMAC mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP). LCL161 enhanced the proapoptotic effects of nilotinib and PKC412, against leukemic disease in vitro and potentiated the activity of both kinase inhibitors against leukemic disease in vivo. |
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