ASK1-IN-1

2411382-24-4

405.41

10 mM in DMSO

MAPK/ERK Pathway

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)^[1]. IC50 & Target: IC50: 138/21 nM (ASK1 in cell and Biochemical assays, respectively)^[1] In Vitro: ASK1-IN-1 (compound 21) has superior CYP inhibition profile and it is also inactive in a hERG assay. ASK1-IN-1 is selected for a kinase selectivity profile against a panel of 468 kinases and it is found to be moderately selective^[1]. In Vivo: ASK1-IN-1 (10 mg/kg; p.o.) covers the cellular IC₅₀/IC₇₀/IC₉₀ at trough in the brain for 12 hours of 50/115/435 mg/kg respectively. ASK1-IN-1 has good biochemical and cellular potency, low clearance and good brain penetration in rodents^[1].