CC-99677

Description: CC-99677 (Gamcemetinib) is a selectively targeted covalent MAPKAPK2 (MK2) inhibitor for autoimmune diseases that translates biochemical potency into cellular potency as demonstrated by potent inhibition of heat shock protein 27 (HSP1) phosphorylation in LPS-activated monocyte THP-27 cells via a nucleophilic aromatic substitution (SNAr) mechanism.CC-99677 in Rat experiments demonstrated potency in both biochemical (IC 50 =156.3 nM) and cellular assays (EC 50 =89 nM). Target: HSP, MAPK. Smiles: CCOCc1cnc(Cl)nc1Oc1ccc2c3c4NC[C@@H](C)NC(=O)c4sc3ccc2n1. References: RAMIREZ V, et al. METHODS OF TREATING A MK2-MEDIATED DISORDER. WO2020236636.