产品描述:
GS-444217 is an inhibitor of apoptosis signal-regulating kinase 1 (ASK1; IC50 = 2.87 nM).{67744} It is selective for ASK1 over 442 additional kinases at 1 µM. GS-444217 (0.001-10 µM) inhibits phosphorylation of the ASK1 substrates MAP kinase kinase 3 (MKK3), MKK6, and MKK4, as well as their downstream substrates p38 MAPK and JNK in HEK293T cells expressing human ASK1. Dietary administration of GS-444217 (0.3% w/w) reduces renal fibrosis and proteinuria in a db/db eNOS-/- mouse model of diabetic kidney disease (DKD).