TBBA highly selective CK2α, Dyrk1A, and NS3 viral helicase inhibitor

TBB (CAS 17374-26-4)

TBB | CAS 17374-26-4 is rated 5.0 out of 5 by 1.
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Synonym: 4,5,6,7-tetrabromobenzotriazole; Casein Kinase II Inhibitor I
Application: A highly selective CK2α, Dyrk1A, and NS3 viral helicase inhibitor
CAS Number: 17374-26-4
Purity: ≥98%
Molecular Weight: 434.71
Molecular Formula: C6HBr4N3
* Refer to Certificate of Analysis for lot specific data (including water content).
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TBB is a cell-permeable benzotriazolo compound that acts as a highly selective ATP/GTP-competitive protein kinase inhibitor. It has been shown to specifically inhibit casein kinase IIα (CK2α) and dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A (Dyrk1A). TBB's strong binding action appears to result from both hydrophobic and van der Walls interactions. Other kinases such as GSK (glycogen synthase kinase), Cdk2 (CDK2) and phosphorylase kinase were inhibited to a lesser extent. TBB has also been shown to inhibit NS3-associated viral helicase activities in hepatitis C virus and West Nile virus. TBB has been used as an apoptotic inducer in Jerkat cells.


References

1. Fromageot, H P., et al., 1977. Adsorption of human erythrocyte surface glycoprotein onto polystyrene latex spheres. The Journal of laboratory and clinical medicine. 90(2): 324-9. PMID: 886218
2. Sarno, S., et al., 2001. Selectivity of 4,5,6,7-tetrabromobenzotriazole, an ATP site-directed inhibitor of protein kinase CK2 ('casein kinase-2'). FEBS letters. 496(1): 44-8. PMID: 11343704
3. Ruzzene, Maria., et al., 2002. Protein kinase CK2 inhibitor 4,5,6,7-tetrabromobenzotriazole (TBB) induces apoptosis and caspase-dependent degradation of haematopoietic lineage cell-specific protein 1 (HS1) in Jurkat cells. The Biochemical journal. 364(Pt 1): 41-7. PMID: 11988074
4. Borowski, Peter., et al., 2003. Halogenated benzimidazoles and benzotriazoles as inhibitors of the NTPase/helicase activities of hepatitis C and related viruses. European journal of biochemistry / FEBS. 270(8): 1645-53. PMID: 12694177
5. Zień, Piotr., et al., 2003. 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): 129-33. PMID: 12788077
6. Sarno, Stefania., et al., 2003. Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA). The Biochemical journal. 374(Pt 3): 639-46. PMID: 12816539
7. Duncan, James S., et al., 2008. An unbiased evaluation of CK2 inhibitors by chemoproteomics: characterization of inhibitor effects on CK2 and identification of novel inhibitor targets. Molecular & cellular proteomics : MCP. 7(6): 1077-88. PMID: 18258654

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), ethanol (20 mM), DMF (~20 mg/ml), and 1:1 solution of DMF:PBS (pH7.2, ~0.5 mg/ml).
Storage :
Store at -20° C
Melting Point :
262-266° C (dec.)
Boiling Point :
552.5° C at 760 mmHg (Predicted)
Density :
2.8 g/cm3 (Predicted)
Refractive Index :
n20D 1.80 (Predicted)
IC50 :
NS3-associated viral helicase activities: IC50 = 1.7 nM ( WNV using DNA substrate); Casein kinase IIα: IC50 = 0.5 µM (human); Casein kinase II: IC50 = 0.9 µM (rat); DYRK1a: IC50 = <1 µM; Casein kinase II: IC50 = 1.6 µM (human)
Ki Data :
Casein kinase IIα: Ki= 400 nM (human)
pK Values :
pKa: 3.87 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
1694
MDL Number :
MFCD06411399
SMILES :
C1(=C(C2=NNN=C2C(=C1Br)Br)Br)Br

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TBB  Product Citations

See how others have used TBB. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 10 total

PMID: # 27033073  Misticone, S. et al. 2016. Methods in molecular biology (Clifton, N.J.). 1388: 95-110.

PMID: # 27693634  Wang, Y. et al. 2016. Cancer Lett. 383: 1-8.

PMID: # 24576828  Kho, DH. et al. 2014. Cancer Res. 74: 2229-37.

PMID: # 23333831  Chuang, KA. et al. 2013. Life sciences. 92: 677-86.

PMID: # 18467326  McDonnell, MA. et al. 2008. J. Biol. Chem. 283: 20149-20158.

PMID: # 18308722  Bachhuber, T. et al. 2008. J. Biol. Chem. 283: 13225-13232.

PMID: # 17289674  Treharne, KJ. et al. 2007. J. Biol. Chem. 282: 10804-10813.

PMID: # 16188887  Remus, D. et al. 2005. J. Biol. Chem. 280: 39740-39751.

PMID: # 15824109  Lolkema, MP. et al. 2005. J. Biol. Chem. 280: 22205-22211.

PMID: # 15159401  Russo, GL. et al. 2004. J. Biol. Chem. 279: 33012-33023.

Citations 1 to 10 of 10 total
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Rated 5 out of 5 by from McDonnell McDonnell, MA. et al. (PubMed 18467326) found that cells preinucbated with TBB, a highly selective CK2 , Dyrk1A, and NS3 viral helicase inhibitor, accelerated the onset of apoptosis in TNF- treated FL5.12 cells. They also found that CK2 inhibition caused the early activation of caspase-9. -SCBT Publication Review
Date published: 2015-05-29
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