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Biological Activity for TBB
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.
Compound Libraries for TBB
Technical Data for TBB
|Storage||Store at +4°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.
Solubility Data for TBB
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for TBB
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 for TBB
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.
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Keywords: TBB, TBB supplier, Selective, cell-permeable, CK2, inhibitors, inhibits, Casein, Kinase, 2, Kinases, NSC231634, NSC, 231634, 2275, Tocris Bioscience
6 Citations for TBB
Citations are publications that use Tocris products. Selected citations for TBB include:
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
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
Wu et al (2014) The BCL2L1 and PGAM5 axis defines hypoxia-induced receptor-mediated mitophagy. Autophagy 10 1712 PMID: 25126723
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
Do you know of a great paper that uses TBB from Tocris? Please let us know.
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Literature in this Area
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