MK2-IN-1

Description: MK2-IN-1 is a novel, potent, non-ATP competitive and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM). 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.

References: ACS Med Chem Lett. 2011 Jun 24; 2(8):632-7.; Bioorg Med Chem Lett. 2012 Jan 15; 22(2):1068-72.

Related CAS#: 1314118-94-9 (HCl salt)