DMAT
| Code | Size | Price |
|---|
| AG-CR1-3654-M001 | 1 mg | £40.00 |
Quantity:
| AG-CR1-3654-M005 | 5 mg | £130.00 |
Quantity:
| AG-CR1-3654-M025 | 25 mg | £370.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Storage:
Short Term: +4°C. Long Term: -20°C
Documents
Further Information
Alternate Names/Synonyms:
2-Dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole; 4,5,6,7-Tetrabromo-N,N-dimethyl-1H-benzimidazol-2-amine
Appearance:
Solid.
CAS:
749234-11-5
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS07
Handling Advice:
Keep cool and dry.
Hazards:
H315, H319, H335
InChi:
InChI=1S/C9H7Br4N3/c1-16(2)9-14-7-5(12)3(10)4(11)6(13)8(7)15-9/h1-2H3,(H,14,15)
InChiKey:
SLPJGDQJLTYWCI-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 749234-11-5. Formula: C9H7Br4N3. MW: 476.8. Synthetic. Potent high affinity ATP-competitive inhibitor of casein kinase II (CK2) (IC50=0.13µM). 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.
MDL:
MFCD08705322
Molecular Formula:
C9H7Br4N3
Molecular Weight:
476.8
Package Type:
Plastic Vial
Precautions:
P302, P352, P304, P340, P305, P351, P338
Product Description:
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.
Purity:
>96% (HPLC)
Signal word:
Warning
SMILES:
CN(C)C1=NC2=C(Br)C(Br)=C(Br)C(Br)=C2N1
Solubility Chemicals:
Soluble in DMSO (10mg/ml).
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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)
Related Products
| Product Name | Product Code | Supplier | CK2 Inhibitor 10 | AG-CR1-3626 | AdipoGen Life Sciences | Summary Details | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| AZD-7762 hydrochloride | SYN-1017 | AdipoGen Life Sciences | Summary Details | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| (+)-JQ1 | SYN-3004 | AdipoGen Life Sciences | Summary Details | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||