A dual inhibitor of CK2 and ERK8
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TMCB is a dual inhibitor of casein kinase 2 (CK2) and ERK8 (IC50 = 0.5 μM for both).[1] It also binds to Pim-1, HIPK2, and DYRK1A (Kis = 8.65, 15.25, and 11.9 μM, 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 μM. TMCB induces apoptosis in Jurkat cells when used at concentrations ranging from 10 to 50 μM.
Reference:
[1]. Pagano, M.A., Bain, J., Kazimierczuk, Z., et al. The selectivity of inhibitors of protein kinase CK2: An update. Biochem. J. 415(3), 353-365 (2008).
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