amg548

AMG-548 is an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ and is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM

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

AMG-548 dihydrochloride 是选择性的、口服具有活力的 p38α 抑制剂，Ki 值为 0.5 nM，对 p38β略有选择性 (Ki=36 nM) 并且对 p38γ 和 p38δ 具有 >1000 倍的选择性。AMG-548 dihydrochloride 对全血 LPS 刺激的 TNFα 表现出抑制作用，IC50 值为 3 nM。AMG-548 dihydrochloride 能够直接抑制酪蛋白激酶 1 (Casein kinase 1) 同种型 δ 和 ε ，并抑制 Wnt 信号传导。

AMG-548 hydrochloride 是选择性的、口服具有活力的 p38α 抑制剂，Ki 值为 0.5 nM，对p38β略有选择性 (Ki=36 nM) 并且对 p38γ 和 p38δ 具有高于1000 倍的选择性。AMG 548 hydrochloride 同时能够有效抑制全血 LPS 刺激的TNFα，IC50值为 3 nM。AMG-548 hydrochloride 能够直接抑制酪蛋白激酶 1 (Casein kinase 1) 同种型 δ 和 ε ，进而对 Wnt 信号传导具有抑制作用。