USP25/28 inhibitor AZ1|2165322-94-9|(AZ1)-陌孚医药/Medlife

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USP25/28 inhibitor AZ1 (Synonyms: AZ1)

目录号: PL02338 纯度: ≥98%

CAS No. :2165322-94-9

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中文名称	USP25/28 inhibitor AZ1
英文名称	USP25/28 inhibitor AZ1
英文别名	USP25/28 inhibitor AZ1;USP25 and 28 inhibitor AZ-1;s8904;2-((5-Bromo-2-((4-fluoro-3-(trifluoromethyl)benzyl)oxy)benzyl)amino)ethan-1-ol;AZ1;Ethanol, 2-[[[5-bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methyl]amino]-;2-[[5-bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methylamino]ethanol;BCP31311;BDBM50514121;E74097;2-(5-Bromo-2-(4-fluoro-3-(trifluoromethyl)benzyloxy)benzylamino)ethanol;2-((5-bromo-2-((4-fluoro-3-(trifluoromethyl)benzyl)oxy)b
Cas No.	2165322-94-9
分子式	C₁₇H₁₆BrF₄NO₂
分子量	422.21
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	USP25/28 inhibitor AZ1 (AZ1) 是一种口服有效，选择性，非竞争性的双重泛素特异性蛋白酶 USP25/28 抑制剂，IC₅₀ 分别为 0.7 μM, 0.6 μM。USP25/28 inhibitor AZ1 可减轻小鼠模型的结肠炎和肿瘤发生。
生物活性	USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC 50 s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model.
性状	Solid
IC50 & Target[1][2]	IC50: 0.7 μM (USP25) and 0.6 μM (USP28)
体内研究(In Vivo)	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 (VP) mice. AZ1 treatment has minimal effect on tumorigenesis in the USP25-deficient background.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Wrigley JD, et al. Identification and Characterization of Dual Inhibitors of the USP25/28 Deubiquitinating EnzymeSubfamily. ACS Chem Biol. 2017 Dec 15;12(12):3113-3125. [2]. Xiao-Meng Wang, et al. The deubiquitinase USP25 supports colonic inflammation and bacterial infection and promotes colorectal cancer. Nature Cancer volume 1, pages811–825(2020).

溶解度数据	In Vitro: DMSO : ≥ 250 mg/mL (592.12 mM)配制储备液

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