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2165322-94-9

中文名称 化合物AZ1
英文名称 AZ-1
CAS 2165322-94-9
分子式 C17H16BrF4NO2
分子量 422.21
MOL 文件 2165322-94-9.mol
更新日期 2025/07/14 21:25:16
2165322-94-9 结构式 2165322-94-9 结构式

基本信息

中文别名
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
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]-
所属类别
生物化工:抑制剂

物理化学性质

沸点478.5±40.0 °C(Predicted)
密度1.488±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: ≥ 250 mg/mL (592.12 mM); Water: < 0.1 mg/mL (insoluble)
酸度系数(pKa)14.74±0.10(Predicted)
形态Solid
颜色White to off-white
InChIInChI=1S/C17H16BrF4NO2/c18-13-2-4-16(12(8-13)9-23-5-6-24)25-10-11-1-3-15(19)14(7-11)17(20,21)22/h1-4,7-8,23-24H,5-6,9-10H2
InChIKeyITHSFXDGKQYOED-UHFFFAOYSA-N
SMILESC(O)CNCC1=CC(Br)=CC=C1OCC1=CC=C(F)C(C(F)(F)F)=C1
化合物AZ1价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/05/22HY-117370化合物AZ1
USP25/28 inhibitor AZ1
2165322-94-91 mg790元
2025/05/22HY-117370化合物AZ1
USP25/28 inhibitor AZ1
2165322-94-95mg1270元
2025/05/22S8904化合物AZ1
USP25/28 inhibitor AZ1
2165322-94-95mg1270元

常见问题列表

生物活性
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。
靶点
TargetValue
USP25
(Cell-free assay)
0.62 μM
USP28
(Cell-free assay)
0.7 μM
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;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.
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