mk2 in 1

MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.

MK2-IN-1 hydrochloride (MK 25) 是一种高效的选择性 MAPKAPK2(MK2)激酶抑制剂，其 IC50值为0.11uM。

Peraquinsin is a MK2 activator that can be utilized in the research of vascular or endothelial barrier disorders and functions as an antihypertensive agent [1].

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)

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。

MMI-0100 是一种细胞渗透性肽抑制剂，抑制丝裂原活化蛋白激酶活化蛋白激酶 II (MK2)。MMI-0100 在体内外减少内膜增生。MMI-0100 抑制IL-6表达而不影响IL-8表达。MMI-0100 抑制纤维化过程，例如静脉移植疾病。

p38α-MK2-IN-1 (Compound 36) 是一种抑制p38α-MK2复合物的抑制剂，IC50为5 nM。此化合物表现出显著的炎症抑制效果，并具备促进关节修复的能力。

MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) 是一种选择性的，可透过神经系统,具有口服活性的的p38α MAPK 抑制剂，Ki 值为 101 nM。MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) 抑制内源性 p38α MAPK 磷酸化活化的神经胶质中内源性底物 MK2 的能力。