| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 138/21 nM (ASK1 in cell and Biochemical assays, respectively) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | ASK1-IN-1 | ||||||||||||
| CAS | 2411382-24-4 | ||||||||||||
| Formula | C19H19N9O2 | ||||||||||||
| Molar Mass | 405.41 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
ASK1-IN-1
CAS: 2411382-24-4 F: C19H19N9O2 W: 405.41
ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC50=138 nM;
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