1. MAPK/ERK Pathway
  2. MAPKAPK2 (MK2)
  3. MK2-IN-1

MK2-IN-1 

Cat. No.: HY-12834
Handling Instructions

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

For research use only. We do not sell to patients.

MK2-IN-1 Chemical Structure

MK2-IN-1 Chemical Structure

CAS No. : 1314118-92-7

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Description

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].

Molecular Weight

472.97

Formula

C₂₇H₂₅ClN₄O₂

CAS No.

1314118-92-7

SMILES

O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)N(C3=CC=C(N4CCNCC4)C=C3)CC5=NC=CC=C5

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

MK2-IN-1MAPKAPK2 (MK2)Mitogen-activated protein kinase activated protein kinase 2MAP kinase activated protein kinase 2MAPK activated protein kinase 2MAPKAP kinase 2Inhibitorinhibitorinhibit

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