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A dual inhibitor of CK2 and ERK8
TMCB is a dual inhibitor of casein kinase 2 (CK2) and ERK8 (IC50 = 0.5 ?M for both).1 It also binds to Pim-1, HIPK2, and DYRK1A (Kis = 8.65, 15.25, and 11.9 ?M, respectively) and inhibits greater than 50% of the activity of five kinases, including CK2, ERK8, and DYRK2, in a panel of 78 kinases at 10 ?M. TMCB induces apoptosis in Jurkat cells when used at concentrations ranging from 10 to 50 ?M.
1.Pagano, M.A., Bain, J., Kazimierczuk, Z., et al.The selectivity of inhibitors of protein kinase CK2: An updateBiochem. J.415(3)353-365(2008)
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