化合物AZ1

生物活性靶点体内研究化合物AZ1 试剂级价格

化合物AZ1

CAS号:2165322-94-9
英文名:AZ-1
中文名:化合物AZ1
CBNumber:CB44668637
分子式:C17H16BrF4NO2
分子量:422.21
MOL File:2165322-94-9.mol

化合物AZ1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 :Store at -20°C
溶解度 :DMSO: ≥ 250 mg/mL (592.12 mM); Water: < 0.1 mg/mL (insoluble)
形态 :Solid
酸度系数(pKa) :14.74±0.10(Predicted)
颜色 :White to off-white
InChI :InChI=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
InChIKey :ITHSFXDGKQYOED-UHFFFAOYSA-N
SMILES :C(O)CNCC1=CC(Br)=CC=C1OCC1=CC=C(F)C(C(F)(F)F)=C1

安全信息

WGK Germany :WGK 3
存储类别 :11 - Combustible Solids

化合物AZ1性质、用途与生产工艺

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
Target Value
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.