2-二甲基氨基-4,5,6,7-四溴苯并咪唑
| 中文名称 | 2-二甲基氨基-4,5,6,7-四溴苯并咪唑 |
|---|---|
| 中文同义词 | 2-二甲基氨基-4,5,6,7-四溴苯并咪唑;4,5,6,7-四溴-N,N-二甲基-1H-苯并[D]咪唑-2-胺;2-二甲基氨基-4,5,6,7-四溴苯并咪唑(DMAT) |
| 英文名称 | CK2 INHIBITOR II |
| 英文同义词 | 4,5,6,7-tetrabroMo-N,N-diMethyl-1H-benzo[d]iMidazol-2-aMine;2-Dimethylamino-4,5,6,7-tetrabromobenzimidazole;DMAT(CK2 Inhibitor);CASEIN KINASE II INHIBITOR;CK2 INHIBITOR;4,5,6,7-tetrabromo-N,N-dimethyl-1H-benzimidazol-2-amine;1H-Benzimidazol-2-amine, 4,5,6,7-tetrabromo-N,N-dimethyl-;DMAT >=98% (HPLC);inhibit,Casein Kinase,DMAT,Inhibitor |
| CAS号 | 749234-11-5 |
| 分子式 | C9H7Br4N3 |
| 分子量 | 476.79 |
| EINECS号 | |
| 相关类别 | Akt;mTOR;PI3K |
| Mol文件 | 749234-11-5.mol |
| 结构式 |  |
2-二甲基氨基-4,5,6,7-四溴苯并咪唑 性质
| 熔点 | >330℃ (Decomposition) |
|---|---|
| 沸点 | 497.7±55.0 °C(Predicted) |
| 密度 | 2.410±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO 中≥23.85 mg/mL；不溶于乙醇；不溶于水 |
| 形态 | 固体 |
| 酸度系数(pKa) | 4.55±0.30(Predicted) |
| 颜色 | 白色至米白色 |
|
CK2 0.13 μM (IC 50 , Human CK2) |
PIM1 0.148 μM (IC 50 ) |
PIM2 1.6 μM (IC 50 ) |
PIM3 0.097 μM (IC 50 ) |
HIPK2 0.37 μM (IC 50 ) |
HIPK3 0.59 μM (IC 50 ) |
DYRK1a 0.41 μM (IC 50 ) |
DYRK2 0.35 μM (IC 50 ) |
DYRK3 1.7 μM (IC 50 ) |
PKD1 0.18 μM (IC 50 ) |
CDK2 0.64 μM (IC 50 ) |
DMAT (1 μM-2.5 μM) DMAT is more efficient in killing antiestrogen resistant cells than parental antiestrogen sensitive MCF-7 cells. DMAT-induced cell death of antiestrogen resistant cells is mediated by caspases. DMAT inhibits CK2 activity but the inhibition is similar in the three cell lines, MCF-7, TAMR-1 and 182R-6. DMAT has effects on H295R cell proliferation at concentrations of 10 -4 and 10 -5 mol/Las compared with the control. DMAT (100 μM) significantly increases apoptosis of H295R cells. DMAT (1 nM-1 μM) significantly decreases aldosterone release into supernatants of 72-h H295R cell cultures as compared with the control. DMAT also inhibits PIM1 by a mechanism which is competitive with respect to ATP, and it is a powerful inhibitor of kinases other than CK2.
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.