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2-Dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole; 4,5,6,7-Tetrabromo-N,N-dimethyl-1H-benzimidazol-2-amine

Chemical

C9H7Br4N3

476.8

749234-11-5

≥96% (HPLC)

Solid.

Soluble in DMSO (10mg/ml).

Determined by 1H-NMR.

SLPJGDQJLTYWCI-UHFFFAOYSA-N

AMBIENT

+4°C

-20°C

Keep cool and dry.

Stable for at least 2 years after receipt when stored at -20°C.

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• Potent high affinity ATP-competitive inhibitor of casein kinase II (CK2) (IC₅₀=0.13µM). Inhibits CK2 in rat liver with >1000-fold greater selectivity for CK2 than for CK1 (IC₅₀=140nM and >200 μM, respectively).
• DYRK1A and DYRK2 inhibitor (IC₅₀= ~0.4µM for both).
• Shown to inhibit additional kinases, such as PIM1, PIM3, HIPK2, HIPK3, PKD1 and CDK2 in the submicromolar range.
• Anticancer agent. Apoptosis inducer in different cancer cell lines.
• Induces reactive oxygen species (ROS) and DNA double strand breaks in tumor cells.
• Induces apoptosis in cells expressing an inhibitor-resistant CK2, by inhibiting quinone reductase 2 (NQO2), binding with similar affinities to the oxidized and reduced forms of NQO2.
• Useful for in vivo studies due to cell permeability and high efficacy in cultured cells and implications in research and treatment of neoplasia and infective diseases, in which CK2 plays a role.

Product References

Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole: M.A. Pagano, et al.; J. Med. Chem. 47, 6239 (2004)

2-Dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole: a novel powerful and selective inhibitor of protein kinase CK2: M.A. Pagano, et al.; BBRC 321, 1040 (2004)

Induction of cell death in antiestrogen resistant human breast cancer cells by the protein kinase CK2 inhibitor DMAT: C.W. Yde, et al.; Cancer Lett. 256, 229 (2007)

The selectivity of inhibitors of protein kinase CK2: an update: M.A. Pagano, et al.; Biochem. J. 415, 353 (2008)

DMAT, an inhibitor of protein kinase CK2 induces reactive oxygen species and DNA double strand breaks: C.C. Schneider, et al.; Oncol. Rep. 21, 1593 (2009)

Anti-neoplastic effect of protein kinase CK2 inhibitor, 2-dimethylamino-4,5,6,7-tetrabromobenzimidazole (DMAT), on growth and hormonal activity of human adrenocortical carcinoma cell line (H295R) in vitro: H. Lawnicka, et al.; Cell Tissue Res. 340, 371 (2010)

Inhibition of experimental HCC growth in mice by use of the kinase inhibitor DMAT: G. Sass, et al.; Int. J. Oncol. 39, 433 (2011)

Quinone reductase 2 is an adventitious target of protein kinase CK2 inhibitors TBBz (TBI) and DMAT: K.K. Leung & B.H. Shilton; Biochemistry 54, 47 (2015)

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