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TBBz

Cat. No. M8823
TBBz Structure
Synonym:

4,5,6,7-Tetrabromo-1H-benzimidazole

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Biological Activity

TBBz is a selective, cell-permeable, ATP-competitive inhibitor of casein kinase 2 (CK2).

Chemical Information
Molecular Weight 433.72
Formula C7H2N2Br4
CAS Number 577779-57-8
Solubility (25°C) DMSO: ≥10 mg/mL at 60 °C
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kevin K K Leung, et al. Quinone reductase 2 is an adventitious target of protein kinase CK2 inhibitors TBBz (TBI) and DMAT

[2] Wei Luo, et al. Inhibition of protein kinase CK2 reduces Cyp24a1 expression and enhances 1,25-dihydroxyvitamin D(3) antitumor activity in human prostate cancer cells

[3] J Tang, et al. Phosphorylation of human La protein at Ser 366 by casein kinase II contributes to hepatitis B virus replication and expression in vitro

[4] Piotr Zien, et al. 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

[5] Piotr Zień, et al. TBBz but not TBBt discriminates between two molecular forms of CK2 in vivo and its implications

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Keywords: TBBz, 4,5,6,7-Tetrabromo-1H-benzimidazole supplier, Casein Kinase, inhibitors, activators

 
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