AMG-548 hydrochloride is an orally active and selective p38α inhibitor (Ki: 0.5 nM) and shows slightly selective over p38β (Ki: 36 nM) and >1000 fold selective against p38γ p38δ. It is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50: 3 nM).
AMG-548 dihydrochloride is an orally active and selective p38α inhibitor (Ki: 0.5 nM) and shows slightly selective over p38β (Ki: 36 nM) and >1000 fold selective against p38γ p38δ. It is also extremely potent in the inhibition of whole blood LPS stimulate
p38 MAPK inhibitor IV is an ATP-competitive inhibitor of p38 MAP kinases with IC50 values of 0.13, 0.55, 5.47, and 8.63 μM for p38α, p38β, p38x, and p38δ, respectively, in vitro.[1] It also inhibits LPS-induced TNF-α and IL-1β cytokine production (IC50s = 22 and 44 nM, respectively) in human peripheral blood mononuclear cells.
p38 MAPK-IN-3 (Compound 2c) is a potent inhibitor of p38α MAPK, displaying antitumor properties by promoting apoptosis and increasing reactive oxygen species (ROS) production [1].
(S)-p38 MAPK inhibitor III is a methylsulfanylimidazole that inhibits p38 MAP kinase (IC50 = 0.90 μM in vitro). It is cell-permeable, potently blocking the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC50s = 0.37 and 0.044 μM, respectively).