| Description |
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].
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| Related Catalog |
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| Target |
IC50: 138/21 nM (ASK1 in cell and Biochemical assays, respectively)[1]
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| 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].
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| 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].
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| References |
[1]. Xin Z, et al. Discovery of CNS-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors. ACS Med Chem Lett. 2020;11(4):485-490. Published 2020 Feb 12.
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