TH-407a (TH407a)

Chemical Structure : TH-407a

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货号: PC-26913Not For Human Use, Lab Use Only.

TH-407a is a potent and selective, reversible, non-competitive inhibitor of ubiquitin-specific peptidase 15 (USP15) with IC50 of 0.76 uM.

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生物&药学活性

TH-407a is a potent and selective, reversible, non-competitive inhibitor of ubiquitin-specific peptidase 15 (USP15) with IC50 of 0.76 uM.
TH-407a inhibits the hydrolysis of Ub-AMC by USP15 in vitro, also inhibits the binding of USP15 to Ub-PA.
TH-407a exhibits negligible inhibition of USP1, USP2, and USP7 at 10 uM.
TH-407a inhibits USP15 via an allosteric regulatory mechanism rather than direct competition with the catalytic site.
TH-407a inhibits breast cancer cell proliferation with IC50 of 19.57 uM and 38.66 uM for MCF-7 and MDA-MB-436 cells, inhibits colony formation, and cancer cell migration.
TH-407a activates the p53 signaling pathway and inhibits the expression of PARP1.
TH-407a (100 mg/kg, oral gavage daily) significantly reduces tumor growth in mice xenografts with MCF-7 and MDA-MB-436 cells.

物理化学性质&存储条件

分子量	354.41
分子式	C22H18N4O
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	naphthalen-2-yl(3-(4-phenyl-1H-1,2,3-triazol-1-yl)azetidin-1-yl)methanone

参考文献

1. Zhang T, et al. Discovery of a potent and selective small-molecule inhibitor of ubiquitin-specific peptidase 15 (USP15) for the treatment of breast cancer. Eur J Med Chem. 2026 May 25;316:119005.

TH-407a (TH407a)

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TH-407a (TH407a)

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