749234-11-5
749234-11-5 结构式
基本信息
4,5,6,7-四溴-N,N-二甲基-1H-苯并[D]咪唑-2-胺
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
物理化学性质
常见问题列表
|
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.