p38a inhibitor 2

p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets[1]. [1]. Raubo P, et al. The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38α MAP kinase inhibitors [published online ahead of print, 2020 Jul 15]. Bioorg Med Chem Lett. 2020;30(18):127412.

CK1-IN-2 (compound Nr.4) 是一种有效的 CK1 抑制剂，对 CK1a、CK1d、CK1e、p38a 的 IC50 值分别为 123、19.8、26.8、74.3 nM，可用于DUX4过表达相关的疾病，如肌肉萎缩症。

CK1-IN-2 (compound Nr.4) hydrochloride 作为CK1抑制剂具有高效性,其对 CK1a、CK1d、CK1e、p38a 的IC50值分别达到 123、19.8、26.8、74.3 nM.