GS-444217

GS-444217 is an inhibitor of apoptosis signal-regulating kinase 1 (ASK1, IC50 = 2.87 nM). 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).Formal Name: 4-(4-cyclopropyl-1H-imidazol-1-yl)-N-[3-(4-cyclopropyl-4H-1,2,4-triazol-3-yl)phenyl]-2-pyridinecarboxamide. CAS Number: 1262041-49-5. Synonyms: Apoptosis Signal-regulating Kinase 1-IN-1, Apoptosis Signal-regulating Kinase 1 Inhibitor 1, ASK1-IN-1, ASK1 Inhibitor 1. Molecular Formula: C23H21N7O. Formula Weight: 411.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Slightly Soluble: 0.1-1 mg/ml. SMILES: O=C(C1=CC(N2C=NC(C3CC3)=C2)=CC=N1)NC4=CC=CC(C5=NN=CN5C6CC6)=C4. InChi Code: InChI=1S/C23H21N7O/c31-23(20-11-19(8-9-24-20)29-12-21(25-13-29)15-4-5-15)27-17-3-1-2-16(10-17)22-28-26-14-30(22)18-6-7-18/h1-3,8-15,18H,4-7H2,(H,27,31). InChi Key: ZGCMQKWOUIMBEP-UHFFFAOYSA-N.