2-二甲基氨基-4,5,6,7-四溴苯并咪唑
- CAS号:749234-11-5
- 英文名:CK2 INHIBITOR II
- 中文名:2-二甲基氨基-4,5,6,7-四溴苯并咪唑
- CBNumber:CB2497369
- 分子式:C9H7Br4N3
- 分子量:476.79
- MOL File:749234-11-5.mol
- 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 :≥23.85 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
- 形态 :solid
- 酸度系数(pKa) :4.55±0.30(Predicted)
- 颜色 :White to off-white
2-二甲基氨基-4,5,6,7-四溴苯并咪唑性质、用途与生产工艺
- 生物活性 DMAT 是一种有效的，特异性的 CK2 抑制剂，IC50 值为 130 nM。
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靶点
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 )
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体外研究
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.
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体内研究
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.
- 公司名称：SIGMA
- 联系电话：--
- 电子邮件：
- 国家：瑞士
- 产品数：6896
- 优势度：91
