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 .
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MK2-IN-1 hydrochloride
CAS number：1314118-94-9(DMSO) molecular formula：C27H26Cl2N4O2
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| Chinese alias | MK2-IN-1盐酸盐 | ||
| English alias | - | ||
| CAS number | 1314118-94-9(DMSO) | molecular formula | C27H26Cl2N4O2 |
| molecular weight | 509.4 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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