MAP3K5/ASK1 Inhibitor

Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC₅₀ of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.

NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a K_i of 500 nM and an IC₅₀ of 3 μM.

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.

ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC₅₀=138 nM; Biochemical IC₅₀=21 nM).

TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC₅₀ of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC₅₀ of 0.51 μM).

ASK1-IN-4 is an ASK1 inhibitor (IC₅₀ = 0.2 μM) that interacts with the ATP binding site of ASK1.

CS17919 is a potent, selective and orally active ASK1 inhibitor with an IC₅₀ of 22.52 nM. CS17919 shows anti-inflammatory and antifibrotic effects. CS17919 can be used for the study of metabolic-related kidney and liver diseases.

N-Acetylgalactosaminyltransferase 4 (GALNT4) is a glycosyltransferase capable of inhibiting the activation of ASK1. By directly binding to ASK1, N-Acetylgalactosaminyltransferase 4 suppresses its N-terminal dimerization and subsequent phosphorylation, leading to robust inactivation of downstream JNK/p38 and NF-κB signals, and thereby improving the prognosis of liver surgery.

ASK1-IN-3 is a potent and selective ASK1 kinase inhibitor with IC₅₀ of 33.8 nM, as well as inhibits several cell cycle regulating kinases. ASK1-IN-3 has strong HepG2 cancer cells apoptosis induction and potent cell cycle arrest activities.

MSC 2032964A is an orally active, selective inhibitor for apoptosis signal-regulating kinase 1(ASK1) with IC₅₀ of 96 nM. MSC 2032964A preserves the visual responses in EAE mice model and exhibits potency in ameliorating the neuroinflammation.

(E/Z)-ASK1-IN-4 is an isomer of ASK1-IN-4 (HY-153761). ASK1-IN-4 is an ASK1 inhibitor (IC₅₀ = 0.2 μM) that interacts with the ATP binding site of ASK1.

ASK1-IN-5 (S-99) is an inhibitor of apoptosis signal-regulated kinase 1 (ASK1) and is useful in the study of autoimmune and neurodegenerative diseases.

JT21-25 (compound 9h) is a potent and selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with IC₅₀ of 5.1 nM.