USP25 and 28 inhibitor AZ-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

USP25 和 28 抑制剂 AZ-1 (AZ1) 是一种有效的、选择性的双重 USP25/28 抑制剂，IC50 分别为 0.7/0.6 uM。

USP25 and 28 inhibitor AZ-1 (AZ1) is a potent, selective, dual USP25/28 inhibitor with IC50 of 0.7/0.6 uM, respectively; shows a high degree of selectivity over other deubiquitinases (USP4,7 etc.); demonstrates target engagement against both USP25 and USP28 in cells, elicits modulation of both the total levels and the half-life of the c-Myc oncoprotein in cells, and also induces apoptosis and inhibits cell viability in a range of cancer cell lines.

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USP25/28 inhibitor AZ1 (AZ1; 40?mg/kg; gavage; daily; for 7?days) protects from dextran sulfate sodium (DSS)-induced weight loss and diarrhea and impaired colon shortening.USP25/28 inhibitor AZ1 (20?mg/kg/day; gavage; 6 times a week in the 1, 3, 6 weeks) treatment significantly reduces tumor numbers in colons. Expression of Wnt-related genes and levels of pSTAT3 are decreased and levels of SOCS3 are increased in tumors. AZ1 gavage does not alleviate DSS-induced colitis in Usp25-/- mice or the spontaneous colitis of Il10-/- mice.USP25/28 inhibitor AZ1 (20?mg/kg/day; gavage; every 3?days from 13-20 weeks) significantly inhibits tumorigenesis in the colon and prolonged the survival of AOM/Vil-Cre;Trp53fl/fl (VP) mice. AZ1 treatment has minimal effect on tumorigenesis in the USP25-deficient background. Animal Model:12-week old male Usp25+/+ and Usp25-/- miceDosage: 40?mg/kg Administration:Gavage; daily; for 7?days Result:Protected from dextran sulfate sodium (DSS)-induced weight loss and diarrhea and impaired colon shortening and potentiated the expression of proinflammatory cytokines and antibacterial peptides in colons of Usp25-/- mice compared to control counterparts.

AZ1

Proteasome/Ubiquitin

DUB

DUB

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2165322-94-9

422.218

C17H16BrF4NO2

>98% (HPLC)

10 mM in DMSO

FC(C1=CC(COC2=CC=C(Br)C=C2CNCCO)=CC=C1F)(F)F

2-((5-bromo-2-((4-fluoro-3-(trifluoromethyl)benzyl)oxy)benzyl)amino)ethan-1-ol

(-20℃)

With Ice Pack

≥ 2 years