Chemical Structure : IAP antagonist Compound A
CAS No.:
908015-92-9
IAP antagonist Compound A
货号: PC-23123Not For Human Use, Lab Use Only.
IAP antagonist Compound A is a highly potent, Smac-mimetic IAP antagonist with equivalent binding affinity to XIAP and cIAP1 in the picomolar range, induces rapid degradation of cIAP1, activates NF-κB signaling via inhibtion of cIAP1 and induces TNFα-dependent apoptosis.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
IAP antagonist Compound A is a highly potent, Smac-mimetic IAP antagonist with equivalent binding affinity to XIAP and cIAP1 in the picomolar range, induces rapid degradation of cIAP1, activates NF-κB signaling via inhibtion of cIAP1 and induces TNFα-dependent apoptosis.
IAP antagonist Compound A competes with Smac for binding to IAPs and also for caspase 9 binding and interacts specifically with the BIR2 and BIR3 domains of cIAP1, cIAP2, and XIAP.
IAP antagonist Compound A (5 nM and 500 nM) exhibits significant killing of Kym1, OVCAR4, and SKOV3 lines.
IAP antagonist Compound A induces rapid degradation of cIAP1 in a binding- and proteasomal-dependent manner.
IAP antagonist Compound A activates NF-κB signaling and induces production of TNFα in an NF-κB-dependent manner in drug-sensitive cell lines.
Brefeldin A and Geldanamycin could blocked cell death induced by compound A.
IAP antagonist Compound A sensitized cells to TNFα-induced cell death.
物理化学性质&存储条件
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分子量
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995.27
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分子式
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C56H76F2N8O6
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(2S,2'S)-N,N'-((2S,2'S)-((2S,2'S)-((1,4-phenylenebis(6-fluoro-1-(2-hydroxyethyl)-1H-indole-2,3-diyl))bis(methylene))bis(pyrrolidine-2,1-diyl))bis(3,3-dimethyl-1-oxobutane-1,2-diyl))bis(2-(methylamino)propanamide)
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参考文献
1. Vince JE, et al. Cell. 2007 Nov 16;131(4):682-93.
