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。

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC 50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis.

Solid

ASK1 32.8 nM (IC50)

ASK1-IN-2 (compound 19) (10 mM; 1 h) inhibits the luciferase reporter activity in AP1-HEK293 cells, with inhibition rate of 95.59%. has not independently confirmed the accuracy of these methods. They are for reference only.

ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) improves dextran sulphate sodium (DSS)-induced ulcerative colitis (UC) in mice.
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.
ASK1-IN-2 (1 mg/kg; i.v.) shows low clearance (CL=1.38 L/h/kg) and moderate half-life (T 1/2 =1.45 h) in rats.
ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUC last =4517 h?ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T 1/2 =2.31 h) in rats. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 250 mg/mL (686.10 mM; Need ultrasonic)配制储备液