2165322-94-9
2165322-94-9 结构式
基本信息
2-[[[5-溴-2-[[4-氟-3-(三氟甲基)苯基]甲氧基]苯基]甲基]氨基]-乙醇
USP25 and 28 inhibitor AZ-1
AZ-1
AZ-1
AZ 1
AZ1
2-((5-bromo-2-((4-fluoro-3-(trifluoromethyl)benzyl)oxy)benzyl)amino)ethanol
Ethanol, 2-[[[5-bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methyl]amino]-
物理化学性质
常见问题列表
| Target | Value |
|
USP25
(Cell-free assay) | 0.62 μM |
|
USP28
(Cell-free assay) | 0.7 μM |
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;Trp53
fl/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. |