化合物AZ1
| 中文名称 | 化合物AZ1 |
|---|---|
| 中文同义词 | 2-[[[5-溴-2-[[4-氟-3-(三氟甲基)苯基]甲氧基]苯基]甲基]氨基]-乙醇;化合物AZ1;USP25/28抑制剂AZ1 |
| 英文名称 | AZ-1 |
| 英文同义词 | Ethanol, 2-[[[5-bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methyl]amino]-;AZ-1;AZ 1;AZ1;2-((5-bromo-2-((4-fluoro-3-(trifluoromethyl)benzyl)oxy)benzyl)amino)ethanol;AZ-1;USP25 and 28 inhibitor AZ-1;USP25/28 inhibitor AZ1;Deubiquitinase,USP-25/28 inhibitor AZ1,USP25/28 inhibitor AZ1,inhibit,AZ 1,Inhibitor,AZ-1,DUBs |
| CAS号 | 2165322-94-9 |
| 分子式 | C17H16BrF4NO2 |
| 分子量 | 422.21 |
| EINECS号 | |
| 相关类别 | 有机化学;中药对照品 |
| Mol文件 | 2165322-94-9.mol |
| 结构式 |  |
化合物AZ1 性质
| 沸点 | 478.5±40.0 °C(Predicted) |
|---|---|
| 密度 | 1.488±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：≥250mg/mL（592.12mM）；水：< 0.1 mg/mL（不溶） |
| 酸度系数(pKa) | 14.74±0.10(Predicted) |
| 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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-117370 | USP25/28 inhibitor AZ1 | 1 mg | 1090元 | |
| 2024/04/30 | S8904 | 化合物AZ1 USP25/28 inhibitor AZ1 | 2165322-94-9 | 5mg | 1270元 |