PF-3644022 is a potent and selective, freely reversible, ATP-competitive inhibitor of MAPKAP2 (MK2) with Ki of 3 nM.
PF-3644022 shows good selectivity against a panel of 200 human kinases.
PF-3644022 potently inhibits TNFα production with similar activity (IC50=160 nM) in U937 cells and hPBMCs, blocks TNFα and IL-6 production in LPS-stimulated human whole blood with IC50 of 1.6 and 10.3 uM, respectively.
PF-3644022 is activite in the rat LPS-induced TNFalpha model and orally efficacious.
