SMTIN-C10

Chemical Structure : SMTIN-C10

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货号: PC-21380Not For Human Use, Lab Use Only.

SMTIN-C10 is a potent, allosteric tumor necrosis factor receptor-associated protein-1 (TRAP1) inhibitor with IC50 of 1.88 uM, by conjugating TPP a C10 linker, and PU-H71.

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生物&药学活性

SMTIN-C10 is a potent, allosteric tumor necrosis factor receptor-associated protein-1 (TRAP1) inhibitor with IC50 of 1.88 uM, by conjugating TPP a C10 linker, and PU-H71.
SMTIN-C10 interacts with the E115 residue in the N-terminal domain through the TPP moiety and subsequently induces structural transition of TRAP1 to a tightly packed closed form.
SMTIN-C10 reduces chaperone activity of TRAP1 more effectively than PU-H71.
SMTIN-C10 shows inhibition of TRAP1 in cancer cells and enhances production of mitochondrial ROS.
SMTIN-C10 (5 mg/kg, i.p., daily) reduces tumor growth significantly in H460-xenograft mice, exhibits superior TRAP1 inhibition and anticancer activity of SMTIN-C10 in vitro and in vivo as compared with other Hsp90 and TRAP1 inhibitors.

物理化学性质&存储条件

分子量	842.80
分子式	C42H46IN5O2PS+
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	(12-(6-amino-8-((6-iodobenzo[d][1,3]dioxol-5-yl)thio)-9H-purin-9-yl)dodecyl)triphenylphosphonium

参考文献

1. Sung Hu, et al. J Med Chem. 2020 Mar 26;63(6):2930-2940.

SMTIN-C10

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物理化学性质&存储条件

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SMTIN-C10

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