化合物AZ1
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- CAS号:
- 2165322-94-9
- 英文名:
- AZ-1
- 英文别名:
- USP25/28 inhibitor AZ1;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]-;Deubiquitinase,USP-25/28 inhibitor AZ1,USP25/28 inhibitor AZ1,inhibit,AZ 1,Inhibitor,AZ-1,DUBs
- 中文名:
- 化合物AZ1
- 中文别名:
- 化合物AZ1;USP25/28抑制剂AZ1;2-[[[5-溴-2-[[4-氟-3-(三氟甲基)苯基]甲氧基]苯基]甲基]氨基]-乙醇
- CBNumber:
- CB44668637
- 分子式:
- C17H16BrF4NO2
- 分子量:
- 422.21
- MOL File:
- 2165322-94-9.mol
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化合物AZ1化学性质
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沸点:
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478.5±40.0 °C(Predicted)
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密度:
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1.488±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: ≥ 250 mg/mL (592.12 mM); Water: < 0.1 mg/mL (insoluble)
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酸度系数(pKa):
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14.74±0.10(Predicted)
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化合物AZ1性质、用途与生产工艺
AZ1是一种非竞争性的泛素特异性蛋白酶25（USP25）和泛素特异性蛋白酶28（USP28） 的双重抑制剂，在Ub-RH110检测中对USP25和USP28的IC50分别0.62 μM和0.7 μM。
| Target | Value |
USP25
(Cell-free assay)
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0.62 μM
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USP28
(Cell-free assay)
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0.7 μM
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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;Trp53
fl/fl
(VP) mice. AZ1 treatment has minimal effect on tumorigenesis in the USP25-deficient background.
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Animal Model:
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12-week old male Usp25
+/+
and Usp25
-/-
mice
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Dosage:
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40 mg/kg
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Administration:
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Gavage; daily; for 7 days
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Result:
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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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化合物AZ1
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
2165322-94-9, 化合物AZ1 相关搜索:
- 药靶配体
- 中药对照品
- 有机化学
- C17H16BrF4NO2
- USP25/28抑制剂AZ1
- 化合物AZ1
- 2-[[[5-溴-2-[[4-氟-3-(三氟甲基)苯基]甲氧基]苯基]甲基]氨基]-乙醇
- 2165322-94-9
- Deubiquitinase,USP-25/28 inhibitor AZ1,USP25/28 inhibitor AZ1,inhibit,AZ 1,Inhibitor,AZ-1,DUBs
- USP25/28 inhibitor AZ1
- USP25 and 28 inhibitor AZ-1
- AZ-1
- 2-((5-bromo-2-((4-fluoro-3-(trifluoromethyl)benzyl)oxy)benzyl)amino)ethanol
- AZ-1;AZ 1;AZ1
- Ethanol, 2-[[[5-bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methyl]amino]-