TRAP-1 | p53 activator | Probechem Biochemicals

Chemical Structure : TRAP-1

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TRAP-1 (TRAP1)

货号: PC-23521Not For Human Use, Lab Use Only.

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生物&药学活性

TRAP-1 is a small molecule chemical inducer of proximity that activates mutant p53, engages mutant p53Y220C and BRD4 in a ternary complex, which potently activates mutant p53 and triggers robust p53 target gene transcription.
TRAP-1 induces a stable interaction between p53Y220C and BRD4. exhibited antiproliferative activity in BxPC-3 (p53Y220C) cells with submicromolar IC50 values (BxPC-3. IC50=0.53 uM).
TRAP-1 induces a mutant-specific ternary complex formation, resulting in a potent and selective antiproliferative effect against p53Y220C bearing cancer cells.
TRAP-1 induces rapid upregulation of p21 and other p53 target genes and inhibits the growth of p53Y220C-expressing cell lines.

物理化学性质&存储条件

分子量	1108.71
分子式	C57H66ClF3N11O3PS
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	(S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-1-(4-((1-(2-(4-((2-(3-((4-(dimethylphosphoryl)phenyl)amino)prop-1-yn-1-yl)-1-(2,2,2-trifluoroethyl)-1H-indol-4-yl)amino)piperidin-1-yl)acetyl)piperidin-4-yl)methyl)piperazin-1-yl)ethan-1-one

参考文献

1. Zhu X, et al. bioRxiv [Preprint]. 2024 Oct 28:2024.10.23.619961.

TRAP-1 (TRAP1)

生物&药学活性

物理化学性质&存储条件

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TRAP-1 (TRAP1)

生物&药学活性

物理化学性质&存储条件

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