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编 号:F274528
分子式:C17H16BrF4NO2
分子量:422.21
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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生物活性:
USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model.

体内研究:
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-/- mice
Dosage: 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.
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