Biochem/physiol Actions

Tetrabromocinnamic acid (TBCA) is a selective cell-permeable ATP-competitive casein kinase CK2 inhibitor with an IC₅₀ of 110 nM, 2-fold selectivity over CK1, and with the advantage of being less active on DYRK1A (IC₅₀ = 24.5 μM) than other CK2 inhibitors suh as DMAT. Elevated levels of CK2 are associated with many cancers and also with tau hyperphosphorylation and neuropathology found in Alzheimer′s disease and other neurodegenerative disorders. In prostate cancer cells TBCA reduced cell proliferation and caused G2/M cell cycle arrest. In isolated squid axoplasms, TBCA also blocked inhibition of fast axonal transport by Aβ oligomers.