MK2-IN-1 (hydrochloride)

1314118-94-9

C27H26Cl2N4O2

DMSO : 100 mg/mL (196.30 mM; Need ultrasonic)

MAPK/ERK Pathway

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 [1] Target: MAPKAPK2(MK2) inhibitor MK2-IN-1 was profiled for kinase selectivity by screening against a broad panel of 150 protein kinases at a concentration of 10 uM, and only CK1gamma3 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 TNFalpha and IL6 secretion. MK2-IN-1 also dose dependently inhibited IL1beta-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 [3].