TBB (Synonyms: NSC 231634, Tetrabromobenzotriazole) |
Catalog No.GC12181
One-Click Copy Product Info
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TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15μM for rat liver CK2.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 17374-26-4
Sample solution is provided at 25 µL, 10mM.
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TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15μM for rat liver CK2[1]. TBB also inhibits three other kinases with less potency: CDK2 (IC50=15.6μM), phosphorylase kinase (IC50=8.7μM) and glycogen synthase kinase 3β (GSK3β) (IC50=11.2μM). All other kinases tested have IC50 values 50-fold greater than that for CK2[2]. TBB is commonly used for studying the role of CK2 in cell signal transduction and gene expression regulation, and can also be applied in the research of related diseases[3-5].
In vitro, after treatment of PC-3 cells with 60μM TBB(24h) followed by a 24h period when cells were cultured without TBB, the viability was considerably lowered, and the time schedule-dependence of the effect was maintained when TBB was administered in combination with Camptothecin (CPT)[6].
In vivo, intraperitoneal injection of TBB (60mg/kg/day for 6 days) reduced retinal neovascularization by approximately 60% in the mouse oxygen-induced retinopathy (OIR) model, with minimal effects on the main vascular tree but marked suppression or elimination of neovascular tufts[7].
References:
[1] Pagano, M. A., Bain, J., Kazimierczuk, Z., Sarno, S., Ruzzene, M., Di Maira, G., Elliott, M., Orzeszko, A., Cozza, G., Meggio, F., & Pinna, L. A. (2008). The selectivity of inhibitors of protein kinase CK2: an update. The Biochemical journal, 415(3), 353–365.
[2] De Moliner, E., Brown, N. R., & Johnson, L. N. (2003). Alternative binding modes of an inhibitor to two different kinases. European journal of biochemistry, 270(15), 3174–3181.
[3] Sarno, S., Reddy, H., Meggio, F., Ruzzene, M., Davies, S. P., Donella-Deana, A., Shugar, D., & Pinna, L. A. (2001). Selectivity of 4,5,6,7-tetrabromobenzotriazole, an ATP site-directed inhibitor of protein kinase CK2 ('casein kinase-2'). FEBS letters, 496(1), 44–48.
[4] Chen, Z., Chen, Q., Huang, J., Gong, W., Zou, Y., Zhang, L., Liu, P., & Huang, H. (2018). CK2α promotes advanced glycation end products-induced expressions of fibronectin and intercellular adhesion molecule-1 via activating MRTF-A in glomerular mesangial cells. Biochemical pharmacology, 148, 41–51.
[5] Zwicker, F., Hauswald, H., Weber, K. J., Debus, J., & Huber, P. E. (2021). In Vivo Evaluation of Combined CK2 Inhibition and Irradiation in Human WiDr Tumours. In vivo (Athens, Greece), 35(1), 111–117.
[6] Orzechowska, E., Kozłowska, E., Staroń, K., & Trzcińska-Danielewicz, J. (2012). Time schedule-dependent effect of the CK2 inhibitor TBB on PC-3 human prostate cancer cell viability. Oncology reports, 27(1), 281–285.
[7] Ljubimov, A. V., Caballero, S., Aoki, A. M., Pinna, L. A., Grant, M. B., & Castellon, R. (2004). Involvement of protein kinase CK2 in angiogenesis and retinal neovascularization. Investigative ophthalmology & visual science, 45(12), 4583–4591.
| Cell experiment [1]: | |
Cell lines | PC-3 cells |
Preparation Method | PC-3 cells were cultured routinely in RPMI-1640 media, respectively, which were supplemented with 10% FBS, penicillin (100U/ml) and streptomycin (100µg/ ml) at 37˚C in a humidified atmosphere of 5% CO2. Cells were seeded at 5x104cells/well in 24-wells plates and cultured for 72h. TBB (final concentration 60µM), Camptothecin (CPT) (final concentration 5.8nM), 2-deoxyglucose (2-DG; final concentration 0.5mM) or tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) (final concentration 13.3ng/ml) were added to the medium individually or in a combination for 24h. Then the medium with the agent was removed and the cells were cultured for another 24h in normal medium. After that, 500µl of MTT mixture (0.5mg/ml in medium without phenol red) was added to each well and incubated for an additional 1h at 37˚C. The formazan crystals were diluted in 250µl of DMSO. The absorbance was measured at 570nm. |
Reaction Conditions | 60μM; 24h |
Applications | TBB reduced the viability of PC-3 cells either alone or combined with anticancer agents CPT or TRAIL when a proper time schedule of the administration is applied. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Proliferative retinopathy in neonatal mice was induced in heterozygous C57BL/6J mice. Mice from the retinopathy group were placed in 75% oxygen at postnatal day 7 and maintained in these conditions with their nursing mothers for 5 days. These mice were then returned to normal air and maintained for another 5 days. Nor-moxic control mice were maintained in normal air for the same duration as test mice and under the same conditions of light cycle and temperature. For in vivo administration, the CK2 inhibitors emodin and TBB were dissolved in PBS (pH 7.2) with 20% polyethylene glycol 400 (PEG 400) and 2% Tween-80. This solvent did not elicit any animal tolerance problems, unlike ethanol or DMSO. Inhibitors were injected intraperitoneally in volumes of 50μL or less per mouse at doses of 15 to 30mg/kg body weight, twice daily from day 11 to day 17. Control mice were injected with PEG-Tween vehicle alone. At the end of the experiment, mice were euthanatized by intraperitoneal injection with tribromoethanol (0.1ml/g body weight).The eyes were enucleated and fixed in 4% paraformaldehyde in 0.1M phosphate buffer (pH 7.4) for 18 hours for further analysis. |
Dosage form | 30 to 60mg/kg/day for 6 days; i.p. |
Applications | TBB reduced retinal neovascularization by approximately 60% in the mouse OIR model with minimal effects on the main vascular tree but marked suppression or elimination of neovascular tufts. |
References: | |
| Cas No. | 17374-26-4 | SDF | |
| Synonyms | NSC 231634, Tetrabromobenzotriazole | ||
| Chemical Name | 4,5,6,7-tetrabromo-2H-benzotriazole | ||
| Canonical SMILES | C1(=C(C2=NNN=C2C(=C1Br)Br)Br)Br | ||
| Formula | C6HBr4N3 | M.Wt | 434.71 |
| Solubility | ≥ 159.2 mg/mL in DMSO, ≥ 10.42 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3004 mL | 11.5019 mL | 23.0038 mL |
| 5 mM | 460.1 μL | 2.3004 mL | 4.6008 mL |
| 10 mM | 230 μL | 1.1502 mL | 2.3004 mL |
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)