4,5,6,7-Tetrabromobenzimidazole (Synonyms: Casein Kinase II Inhibitor XII,TBBz) |
Catalog No.GC16960 |
Le 4,5,6,7-tétrabromobenzimidazole est un inhibiteur sélectif et compétitif de la CK2 (caséine kinase 2) pour l'ATP.
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Cas No.: 577779-57-8
Sample solution is provided at 25 µL, 10mM.
Ki: 0.5-1 μM
4,5,6,7-Tetrabromobenzimidazole is a CK2 inhibitor.
Casein kinase 2 (CK2), a constitutive protein kinase involved in many signal transduction pathways, is known to be able to negatively regulate apoptosis, and its activity is increased in various proliferating tissues and tumors.
In vitro: Previous study found that like the reported 4,5,6,7-tetrabromobenzotriazole (TBBt), the structurally related 4,5,6,7-tetrabromobenzimidazole (TBBz) was a selective ATP-competitive inhibitor of protein kinase CK2 from various sources including yeast, rat liver, Neurospora crassa and Candida tropicalis, with K(i) values in the range 0.5-1 μM. TBBz was found to virtually inactive vs. PKA, PKC, and a very weak inhibitor of protein kinase CK1. TBBt was noted to be a more effective inhibitor of PK60S than of yeast CK2; by contrast, TBBz was a relatively feeble inhibitor of PK60S, thus more selective than TBBt vs. CK2 in yeast cells. Therefore, similar to TBBt, TBBz could be regarded as an additional lead compound for development of more potent inhibitors of CK2 [1].
In vivo: Up to now, therer is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Zien, P. ,Bretner, M.,Zastapilo, K., et al. Selectivity of 4,5,6,7-tetrabromobenzimidazole as an ATP-competitive potent inhibitor of protein kinase CK2 from various sources. Biochemical and Biophysical Research Communications 306(1), 129-133 (2003).
Cas No. | 577779-57-8 | SDF | |
Synonymes | Casein Kinase II Inhibitor XII,TBBz | ||
Chemical Name | 4,5,6,7-tetrabromo-1H-benzimidazole | ||
Canonical SMILES | BrC1=C2C(N=CN2)=C(Br)C(Br)=C1Br | ||
Formula | C7H2Br4N2 | M.Wt | 433.7 |
Solubility | DMSO: Soluble,Ethanol: Soluble | 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 | 2.3057 mL | 11.5287 mL | 23.0574 mL |
5 mM | 0.4611 mL | 2.3057 mL | 4.6115 mL |
10 mM | 0.2306 mL | 1.1529 mL | 2.3057 mL |
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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 ddH2O, 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.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
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