mk2 phosphorylation

CMPD1 是非 ATP 竞争性 p38 MAPK 介导的 MK2磷酸化选择性抑制剂(Ki:330 nM)。

Ralimetinib selectively inhibits phosphorylation of MK2 (Thr334) and has no effect on phosphorylation of p38α MAPK, JNK, ERK1 2, c-Jun, ATF2, or c-Myc. Ralimetinib is an effective and selective, ATP-competitive inhibitor of p38 MAPK α β (IC50s: 5.3 and 3.

Potent and selective p38α and p38β degrader (DC50 < 50 nM). Displays no significant degradation of p38γ, p38δ, JNK1/2 or ERK1/2. Inhibits phosphorylation of MK2 in UV-treated cancer cells and LPS-stimulated bone marrow-derived macrophages (BMDM). Exhibits similar effect to p38α gene knockout in BBL358 cells. Active in vivo.

CC-99677 (Gamcemetinib) 是一种一种用于自身免疫性疾病的选择性靶向共价MAPKAPK2(MK2)抑制剂，通过亲核芳族取代(SNAr)机制将生化效力转化为LPS活化的单核细胞THP-27细胞中热休克蛋白27(HSP1)磷酸化的有效抑制所显示的细胞效力。CC-99677 在大鼠实验中展现出在生化(IC 50 =156.3 nM)和细胞检测(EC 50 =89 nM)中均有

MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a potent and selective inhibitor of p38α MAPK, with a Ki value of 101 nM. It exhibits excellent CNS penetration and oral bioavailability. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) effectively suppresses the phosphorylation of MK2, a substrate of endogenous p38α MAPK, in activated glial cells.

(R)-STU104 是一种新型 TAK1-MKK3 蛋白-蛋白相互作用 （PPI）抑制剂，抑制 TNF-α，通过与 MKK3 结合并破坏TAK1磷酸化MKK3来抑制TAK1 MKK3 p38 MnK1 MK2 elF4E信号通路。(R)-STU104 是治疗溃疡性结肠炎的候选化合物。

MK2-IN-5为Mk2的假底物，Ki值为8 μM。该化合物针对MAPK通路内的蛋白相互作用域，并能抑制HSP25与HSP27的磷酸化。