2411382-24-4

2411382-24-4 structure
2411382-24-4 structure
  • Name: CAY10756
  • Chemical Name: ASK1-IN-1
  • CAS Number: 2411382-24-4
  • Molecular Formula: C19H19N9O2
  • Molecular Weight: 405.41
  • Catalog: Signaling Pathways MAPK/ERK Pathway p38 MAPK
  • Create Date: 2020-08-08 16:56:57
  • Modify Date: 2024-01-16 19:05:12
  • 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].

Name ASK1-IN-1
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].
Related Catalog
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].
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.

Molecular Formula C19H19N9O2
Molecular Weight 405.41