Birinapant是一种二价Smac模拟物, 是 XIAP 和 cIAP1 的强效拮抗剂,Kd 值分别为45 nM和小于1 nM。
Description | Birinapant, a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. | ||||||||||||||||
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IC50 & Target | Kd: 45 nM (XIAP), <1 nM (cIAP1) | ||||||||||||||||
In Vitro | Birinapant causes significant degradation of cIAP1 and 2. Birinapant + TRAIL-treated cells show increased levels of active caspase-8 and caspase-3, as well as PARP cleavage, over single agents within 4 h of treatment, indicative of apoptosis-mediated cell death. Birinapan significantly decreases the viability of SUM190 cells in a dose-dependent manner. Birinapant treatment in the XIAP knockdown cell line (SUM190 shXIAP) causes an overall reduction in viability at lower doses (30-300 nM)[1]. Birinapant causes apoptosis in the sensitive cells. Birinapant in conbination with TNF-α, causes PARP cleavage in 451Lu and WM1366 cell lines[2]. Birinapant induces time-course of caspase-3 activation in HCT116 human colon carcinoma and MDA-MB-231 human breast adenocarcinoma cells[3]. | ||||||||||||||||
In Vivo | |||||||||||||||||
Solvent & Solubility | In Vitro: DMSO : ≥ 40 mg/mL (49.57 mM) H2O : < 0.1 mg/mL (insoluble) * "≥" means soluble, but saturation unknown. Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. In Vivo:
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References | |
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