MK2-IN-1 hydrochloride

MK2-IN-1盐酸盐

MK2-IN-1 hydrochloride

M656517-1ml

1ml

10mM in DMSO

充氩,-80℃储存

超低温冰袋运输

MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.IC50 value: 0.11 uM Target: MAPKAPK2(MK2) inhibitorMK2-IN-1 was profiled for kinase selectivity by screening against a broad panel of 150 protein kinases at a concentration of 10 μM, and only CK1γ3 was significantly inhibited at greater than 50%. MK2-IN-1 inhibited pro-inflammatory cytokine secretion from the human THP1 acute monocytic leukemia cell line, causing dose-dependent inhibition of LPS-stimulated TNFα and IL6 secretion. MK2-IN-1 also dose dependently inhibited IL1β-stimulated matrixmetalloprotease (MMP)13 secretion from the SW1353 chondrosarcoma cell line and human primary chondrocyte cultures. Of note, given its high degree of selectivity, our data suggest that MK2-IN-1 may be an excellent pharmacologic tool for specifically exploring and validating MK2 biology .

MK2-IN-1 hydrochloride 是一种强效的 MAPKAPK2(MK2) 选择性抑制剂（IC50=0.11 uM），具有非 ATP 竞争性结合模式：MAPKAPK2(MK2) 抑制剂 （nMK2-IN-1 是通过筛选对

1314118-94-9(DMSO)

C27H26Cl2N4O2

509.4 g/mol

C1CN(CCN1)C2=CC=C(C=C2)N(CC3=CC=CC=N3)C(=O)C4=CC=C(O4)C5=CC=C(C=C5)Cl.Cl

包含CDK，MAPK，GSK3，CLK家族