CAY10756

Names

[ Name ]:
CAY10756

Biological Activity

[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]:

Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK

Research Areas >> Inflammation/Immunology

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₁₉N₉O₂

[ Molecular Weight ]:
405.41