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TBB is a cell-permeable, selective inhibitor of casein kinase-2 (CK2) (IC50 = 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively). Exhibits modest discrimination between CK2 subunits, with Ki values ranging from 80 nM to 210 nM. Acts in an ATP/GTP-competitive manner and displays one to two orders of magnitude selectivity over a panel of 33 protein kinases.
TBB is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 434.71. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.3 mL||11.5 mL||23 mL|
|5 mM||0.46 mL||2.3 mL||4.6 mL|
|10 mM||0.23 mL||1.15 mL||2.3 mL|
|50 mM||0.05 mL||0.23 mL||0.46 mL|
References are publications that support the biological activity of the product.
Sarno et al (2001) Selectivity of 4,5,6,7-tetrabromobenzotriazole, an ATP site-directed inhibitor of protein kinase CK2 ('casein kinase-2'). FEBS Lett. 496 44 PMID: 11343704
Pagano et al (2004) Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J.Med.Chem. 47 6239 PMID: 15566294
Zien et al (2005) Tetrabromobenzotriazole (TBBt) and tetrabromobenzimidazole (TBBz) as selective inhibitors of protein kinase CK2: evaluation of their effects on cells and different molecular forms of human CK2. Biochim.Biophys.Acta. 1754 271 PMID: 16203192
If you know of a relevant reference for TBB, please let us know.
Keywords: TBB, TBB supplier, Selective, cell-permeable, CK2, inhibitors, inhibits, Casein, Kinase, 2, Kinases, NSC231634, NSC, 231634, 2275, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for TBB include:
Korb et al (2015) BET protein Brd4 activates transcription in neurons and BET inhibitor Jq1 blocks memory in mice. Sci Rep 18 1464 PMID: 26301327
Navasa et al (2015) Ikaros mediates the DNA methylation-independent silencing of MCJ/DNAJC15 gene expression in macrophages. J Urol 5 14692 PMID: 26419808
Bartley et al (2016) Mammalian FMRP S499 Is Phosphorylated by CK2 and Promotes Secondary Phosphorylation of FMRP. Eneuro 3 PMID: 27957526
Buchanan et al (2010) Facilitation of long-term potentiation by muscarinic M(1) receptors is mediated by inhibition of SK channels. Neuron 68 948 PMID: 21145007
Lezmy (2017) M-current inhibition rapidly induces a unique CK2-dependent plasticity of the axon initial segment. Proc Natl Acad Sci U S A 114 E10234 PMID: 29109270
Wu et al (2014) The BCL2L1 and PGAM5 axis defines hypoxia-induced receptor-mediated mitophagy. Autophagy 10 1712 PMID: 25126723
Do you know of a great paper that uses TBB from Tocris? Please let us know.
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