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Chemical Structure
Chemical Structure
Chemical Structure

DMAT [749234-11-5]

Research Use Only
AG-CR1-3654
AdipoGen Life Sciences
CAS Number749234-11-5
Product group Chemicals
Estimated Purity>95%
Molecular Weight476.8
Price on request
Packing Size
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    DMAT [749234-11-5]
  • Delivery Days Customer
    10
  • CAS Number
    749234-11-5
  • Certification
    Research Use Only
  • Estimated Purity
    >95%
  • Hazard Information
    Non-hazardous,Warning
  • Molecular Formula
    C9H7Br4N3
  • Molecular Weight
    476.8
  • Scientific Description
    Chemical. CAS: 749234-11-5. Formula: C9H7Br4N3. MW: 476.8. Synthetic. Potent high affinity ATP-competitive inhibitor of casein kinase II (CK2) (IC50=0.13microM). Inhibits CK2 in rat liver with >1000-fold greater selectivity for CK2 than for CK1 (IC50=140nM and >200 microM, respectively). DYRK1A and DYRK2 inhibitor (IC50= ~0.4microM 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. - Potent high affinity ATP-competitive inhibitor of casein kinase II (CK2) (IC50=0.13microM). Inhibits CK2 in rat liver with >1000-fold greater selectivity for CK2 than for CK1 (IC50=140nM and >200 microM, respectively). DYRK1A and DYRK2 inhibitor (IC50= ~0.4microM 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.
  • SMILES
    CN(C)C1=NC2=C(Br)C(Br)=C(Br)C(Br)=C2N1
  • Storage Instruction
    2°C to 8°C,-20°C
  • UNSPSC
    12352200

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)