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Activation of the p38/mitogen-activated protein kinase-activated protein kinase 2 (MAPKAPK2 or MK2) pathway has been implicated in promoting pro-inflammatory cytokine production and related inflammatory diseases. MK2 inhibitor IV is a highly selective, non-ATP competitive MK2 inhibitor with an IC50 value of 0.11 μM.1 MK2 inhibitor IV has been shown to inhibit pro-inflammatory cytokine secretion from the human THP-1 acute monocytic leukemia cell line, causing inhibition of LPS-stimulated TNF-α (IC50 = 4.4 μM) and IL-6 (IC50 = 5.2 μM) secretion.1 It can also inhibit IL-1β-stimulated matrixmetalloprotease 13 secretion from the SW1353 chondrosarcoma cell line (IC50 = 5.7 μM) and human primary chondrocyte cultures (IC50 = 2.2 μM).1
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1. Discovery and hit-