Uses
Casein Kinase II Inhibitor III is a casein kinase 2 inhibitor. A protein kinase inhibitors used to elucidate cellular signaling pathways.
Biological Activity
tetrabromocinnamic acid (tbca) is a new class of specific protein kinase ck2 inhibitors [1].protein kinases have been involved in catalyzing the phosphorylation of serine, threonine and tyrosine residues in protein substrates that play dominant roles in controlling nearly all cellular functions. the ser/thr-specific protein kinase ck2 has been implicated in signal transduction, gene expression, dna repair, rna and protein synthesis. ck2 is invariably elevated in a wide spectrum of tumours [1].
in vitro
tbca was a selective, cell-permeable inhibitor of ck2 with an ic50 of 0.11 μm. the ki value was 77 nm. tbca showed minimal effect on a panel of 28 other kinases. tbca induced cell death in jurkat adult t cell leukemia cells with an dc50 of 7.7 μm [1]. tbca dose-dependently inhibited platelet aggregation and secretion induced by various agonists including 2-mesadp, aypgkf, sfllrn, and crp [2]. tbca also significantly inhibited agonist-induced thromboxane a2 (txa2) generation and erk phosphorylation. tbca significantly inhibited platelet spreading on immobilized fibrinogen surface and clot retraction mediated by integrin αiibβ3 signaling [2].
References
[1] pagano m a, poletto g, di maira g, et al. tetrabromocinnamic acid (tbca) and related compounds represent a new class of specific protein kinase ck2 inhibitors[j]. chembiochem, 2007, 8(1): 129-139.
[2] ryu s y, kim s. evaluation of ck2 inhibitor (e)-3-(2, 3, 4, 5-tetrabromophenyl) acrylic acid (tbca) in regulation of platelet function[j]. european journal of pharmacology, 2013, 720(1): 391-400.
