TC ASK 10

Description

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.

Uses

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.

in vivo

IC 50

ASK1: 14 nM (IC₅₀)

storage

Desiccate at RT

References

[1] YOSHITO TERAO. Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors[J]. Bioorganic & Medicinal Chemistry Letters, 2012, 22 24: Pages 7326-7329. DOI: 10.1016/j.bmcl.2012.10.084