ASK1 inhibitor 10 is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1; IC50 = 14 nM). It is selective for ASK1 over ASK2 (IC50 = 510 nM) as well as MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, and B-RAF (IC50s = >10,000 nM for all). It inhibits streptozotocin-induced increases in JNK and p38 phosphorylation in INS-1 pancreatic β cells in a concentration-dependent manner.
TC ASK 10 is a potent ASK1 inhibitor. It displays selectivity for ASK1 over other kinases including ASK2, MEKK1, TAK1, IKKβ, ERK1, JNK1, p38α, GSK-3β, PKCθ and B-raf. It blocks downstream JNK1/p38 phosphorylation in cells.
