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CBI1

Chemical Structure : CBI1

CAS No.:

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CBI1 (Covalent BAX inhibitor 1)

货号: PC-22105Not For Human Use, Lab Use Only.

Covalent BAX inhibitor 1 (CBI1) is a specific, covalent BAX inhibitor selectively derivatizes BAX at Cys126 and inhibits BAX activation by triggering ligands or point mutagenesis.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Covalent BAX inhibitor 1 (CBI1) is a specific, covalent BAX inhibitor selectively derivatizes BAX at Cys126 and inhibits BAX activation by triggering ligands or point mutagenesis.
CBI1 is not an activator of BAX.
CBI1 demonstrates potent dose-responsive blockade of BAX-mediated liposomal poration upon triggering by the physiologic tBID ligand in liposomal release assay.
CBI1 acts at an upstream control point, specifically the conformational activation step of ligand-triggered monomeric BAX.
CBI1 blocks t-2-hex lipidation and oligomerization of BAX, inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex.
CBI1 not only competes for C126 derivatization to block t-2-hex-mediated BAX sensitization but also independently restrains BAX by stabilizing key structures of its monomeric architecture.

物理化学性质&存储条件

分子量 415.37
分子式 C15H19BrN4OS2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(3-((2-aminoethyl)disulfanyl)propyl)-3-(4-bromophenyl)-1H-pyrazole-5-carboxamide

参考文献

1. Matthew W McHenry, et al. Nat Chem Biol. 2024 Jan 17. doi: 10.1038/s41589-023-01537-6.

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