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Request The Product List ofMAPKAPK2 (MK2) MAPKAPK2 (MK2)

Cat. No. Product Name CAS No. Information
PC-70143

PF-3644022

1276121-88-0

PF-3644022 is a potent and selective, freely reversible, ATP-competitive inhibitor of MAPKAP2 (MK2) with Ki of 3 nM; shows good selectivity against a panel of 200 human kinases; potently inhibits TNFα production with similar activity (IC50=160 nM) in U937 cells and hPBMCs, blocks TNFα and IL-6 production in LPS-stimulated human whole blood with IC50 of 1.6 and 10.3 uM, respectively; activite in the rat LPS-induced TNFalpha model and orally efficacious.

PC-43244

MK2-IN-1 hydrochloride

1314118-94-9 MK2-IN-1 is a potent, selecitve, non-ATP competitive MAPKAPK2(MK2) inhibitor with IC50 of 0.11 uM; shows excellent kinase selectivity against a broad panel of 150 protein kinases at 10 μM with only on exception of CK1γ3 >50 % inhibition; inhibits pro-inflammatory cytokine secretion from the human THP1 acute monocytic leukemia cell line, causing dose-dependent inhibition of LPS-stimulated TNFα and IL6 secretion; also dose dependently inhibits IL1β-stimulated MMP13 secretion from the SW1353 chondrosarcoma cell line and human primary chondrocyte cultures.
PC-43243

MK2-IN-1

1314118-92-7 MK2-IN-1 is a potent, selecitve, non-ATP competitive MAPKAPK2(MK2) inhibitor with IC50 of 0.11 uM; shows excellent kinase selectivity against a broad panel of 150 protein kinases at 10 μM with only on exception of CK1γ3 >50 % inhibition; inhibits pro-inflammatory cytokine secretion from the human THP1 acute monocytic leukemia cell line, causing dose-dependent inhibition of LPS-stimulated TNFα and IL6 secretion; also dose dependently inhibits IL1β-stimulated MMP13 secretion from the SW1353 chondrosarcoma cell line and human primary chondrocyte cultures.
PC-70147

MK2 inhibitor III

1186648-22-5 A potent, cell-permeable inhibitor of MK2 with IC50 of 8.5 nM; less potently blocks MK3 and MK5 (IC50s=210 and 81 nM, respectively) and is weak or inactive against several other kinases, including P38 MAPKs; prevents LPS-induced synthesis of TNF-α in human monocyte-like U937 cells with IC50 of 4.4 uM.
PC-70144

MK2-IN-28

1355617-50-3 A potent and selective, non-ATP competitive, allosteric MAPKAPK2/3 (MK2/3) inhibitor with IC50 of 8 nM for MK2, hTNFα EC50 of 0.31 uM; inhibits both MK2 and MK3, and has no or little effect on the other kinases; ameliorates glucose homeostasis by suppressing excessive HGP and enhancing insulin signaling in obese mice.

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