TBCA
(Synonyms: Casein Kinase II Inhibitor III,Tetrabromocinnamic Acid) 目录号 : GC14181
An inhibitor of casein kinase 2
Cas No.:934358-00-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1566 mL | 10.7828 mL | 21.5657 mL |
| 5 mM | 0.4313 mL | 2.1566 mL | 4.3131 mL |
| 10 mM | 0.2157 mL | 1.0783 mL | 2.1566 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。