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TBCA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TBCA图片
CAS NO:934358-00-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
TBCA 是一种高度选择性的 CK2(酪蛋白激酶 II)抑制剂,IC50 为 110 nM,Ki 为 77 nM。 TBCA 对 CK2 的选择性高于对 CK1、DYRK1A 和一组 27 种其他激酶的选择性。
Cas No.934358-00-6
别名Casein Kinase II Inhibitor III,Tetrabromocinnamic Acid
化学名(2E)-3-(2,3,4,5-tetrabromophenyl)-2-propenoic acid
Canonical SMILESBrC1=C(Br)C(Br)=C(Br)C=C1/C=C/C(O)=O
分子式C9H4Br4O2
分子量463.7
溶解度≤1mg/ml in ethanol;2mg/ml in DMSO;5mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.