MK-2 Inhibitor III is a cell-permeable pyrrolopyridinyl compound that acts as a potent, selective, and ATP-biniding site-targeting MK-2/MAPKAP-K2 inhibitor (IC50 = 8.5, 81, and 210 nM agaisnt MAPKAPK-2 (MK-2), PRAK(MK-5), and 3pK(MK-3), respectively), while exhibiting much less or no activity against 8 other commonly studied kinases. Shown to suppress LPS-induced TNF-α production in U937 cells (IC50 = 4.4 μM).
Anderson, D.R., et al. 2007. J. Med. Chem. 50, 2647.
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Rated 5 out of
Soukup et alSoukup et al. (PubMed ID 26078274) found that MK-2 Inhibitor III inactivated MK2-mediated p38 inhibition and enabled dendritic cells to strengthen proinflammatory mechanisms by potentiating IL-1 -mediated Th1 activity in mice with encephalomyelitis. -SCBT Publication Review
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