| Identification | Back Directory | [Name]
CK2 INHIBITOR II | [CAS]
749234-11-5 | [Synonyms]
DMAT >=98% (HPLC)
DMAT(CK2 Inhibitor)
CASEIN KINASE II INHIBITOR;CK2 INHIBITOR
2-Dimethylamino-4,5,6,7-tetrabromobenzimidazole
4,5,6,7-tetrabromo-N,N-dimethyl-1H-benzimidazol-2-amine
1H-Benzimidazol-2-amine, 4,5,6,7-tetrabromo-N,N-dimethyl-
4,5,6,7-tetrabroMo-N,N-diMethyl-1H-benzo[d]iMidazol-2-aMine | [Molecular Formula]
C9H7Br4N3 | [MDL Number]
MFCD08705322 | [MOL File]
749234-11-5.mol | [Molecular Weight]
476.79 |
| Chemical Properties | Back Directory | [Melting point ]
>330℃ (Decomposition) | [Boiling point ]
497.7±55.0 °C(Predicted) | [density ]
2.410±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥23.85 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O | [form ]
solid | [pka]
4.55±0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
DMAT is a cell-permeable inhibitor of casein kinase 2 (CK2; IC50 = 0.13 μM). It also inhibits Pim-1, Pim-3, HIPK2, and HIPK3 (IC50s = 0.15, 0.097, 0.37, and 0.59 μM, respectively). DMAT blocks cell growth and induces cell death in cancer cells, both in culture and in mouse xenografts. | [Uses]
2-Dimethylamino-4,5,6,7-tetrabromobenzimidazole is a novel powerful and selective inhibitor of protein kinase CK2. | [in vivo]
DMAT application in vivo reduces tumor growth in a xenotransplant model by interference with tumor cell proliferation. Biochemical parameters and histology following DMAT administration revealed no alterations in liver tissue[4]. | [IC 50]
CK2: 0.13 μM (IC50, Human CK2); PIM1: 0.148 μM (IC50); PIM2: 1.6 μM (IC50); PIM3: 0.097 μM (IC50); HIPK2: 0.37 μM (IC50); HIPK3: 0.59 μM (IC50); DYRK1a: 0.41 μM (IC50); DYRK2: 0.35 μM (IC50); DYRK3: 1.7 μM (IC50); PKD1: 0.18 μM (IC50); CDK2: 0.64 μM (IC50) | [storage]
Store at -20°C | [References]
[1] MARIO A PAGANO. The selectivity of inhibitors of protein kinase CK2: an update.[J]. Biochemical Journal, 2008: 353-365. DOI: 10.1042/bj20080309
[2] HANNA LAWNICKA. 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.[J]. Cell and Tissue Research, 2010, 340 2: 371-379. DOI: 10.1007/s00441-010-0960-1
[3] GABRIELE SASS. Inhibition of experimental HCC growth in mice by use of the kinase inhibitor DMAT.[J]. International journal of oncology, 2011, 39 2: 433-442. DOI: 10.3892/ijo.2011.1037
[4] CHRISTINA WESTMOSE YDE . Induction of cell death in antiestrogen resistant human breast cancer cells by the protein kinase CK2 inhibitor DMAT[J]. Cancer letters, 2007, 256 2: Pages 229-237. DOI: 10.1016/j.canlet.2007.06.010 |
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