ASK1-IN-2 是一种有效的，具有口服活性的凋亡信号调节激酶 1 (ASK1) 抑制剂，IC50 值为 32.8 nM。ASK1-IN-2 可用于溃疡性结肠炎的研究。
货号:ajcx33700
CAS:2541792-70-3
分子式:C19H17FN6O
分子量：364.38
溶解度:DMSO : 250 mg/mL (686.10 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis[1].

ASK1-IN-2 (compound 19) (10 mM; 1 h) inhibits the luciferase reporter activity in AP1-HEK293 cells, with inhibition rate of 95.59%[1].

ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) improves dextran sulphate sodium (DSS)-induced ulcerative colitis (UC) in mice[1].ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) blocks ASK1-p38/JNK signaling pathways and reduces inflammatory cytokine levels in DSS-induced mouse colon tissues[1].ASK1-IN-2 (1 mg/kg; i.v.) shows low clearance (CL=1.38 L/h/kg) and moderate half-life (T1/2=1.45 h) in rats[1].ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUClast=4517 h•ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T1/2=2.31 h) in rats[1].

[1]. Hou S, et, al. Structure-based discovery of 1H-indole-2-carboxamide derivatives as potent ASK1 inhibitors for potential treatment of ulcerative colitis. Eur J Med Chem. 2020 Dec 24;211:113114.