TBCA

- Overview
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    Background
    
    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].
    
    [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.
- Properties
  - Alternative Name
    
    Casein Kinase II Inhibitor III,Tetrabromocinnamic Acid; (2E)-3-(2,3,4,5-tetrabromophenyl)-2-propenoic acid
    
    CAS Number
    
    934358-00-6
    
    Molecular Formula
    
    C9H4Br4O2
    
    Molecular Weight
    
    463.7
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤1mg/ml in ethanol;2mg/ml in DMSO;5mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

TBCA

Background

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