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MK2-IN-1

CAS No. : 1314118-92-7

Biological Activity：MK2-IN-1 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 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 [3].

Research Area：Cancer

Targets：MAPKAPK2 (MK2)

Related Small Molecules:CMPD1;MK2-IN-1 hydrochloride;RMM-46;Zunsemetinib;DB1113;Tpl2 Kinase Inhibitor 1;MMI-0100;MK2-IN-4;CC-99677;MK2-IN-3 hydrate;Norartocarpetin;PF-3644022

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