中文名 | TBB |
英文名 | TBB |
别名 | 7-四溴苯并三唑 7-四溴-1H-苯并三唑 4,5,6,7-四溴苯并三唑 4,5,6,7-四溴苯基三唑 蛋白激酶CK2抑制剂(TBB) 4,5,6,7-四溴-1H-苯并三唑 TBB(4,5,6,7-四溴-1H-苯并三唑) 4,5,6,7-四溴苯并三唑, 选择性细胞渗透性酪蛋白激酶2(CK2)抑制剂 |
英文别名 | 6 5 4 TBB TBBT NSC 231634 7-TETRABROMO- 7-tetrabromo- 1H-BENZOTRIAZOLE TBB (ENZYME INHIBITOR) 4,5,6,7-Tetrabromo-1H-benzotriazole 4,5,6,7-Tetrabromo-2-azabenzimidazole, 4,5,6,7-Tetrabromobenzotriazole, NSC 231634, TBBt |
CAS | 17374-26-4 |
化学式 | C6HBr4N3 |
分子量 | 434.71 |
密度 | 2.840±0.06 g/cm3(Predicted) |
熔点 | 262-266°C |
沸点 | 552.5±45.0 °C(Predicted) |
溶解度 | DMSO: 28 mg/mL |
酸度系数 | 3.87±0.40(Predicted) |
存储条件 | 2-8°C |
外观 | 固体 |
颜色 | white |
最大波长(λmax) | ['300nm(MeOH)(lit.)'] |
MDL号 | MFCD06411399 |
体外研究 | Investigation of the inhibitory power of TBB with a panel of 33 protein kinases shows highest potency for CK2 (casein kinase 2) (human CK2: IC 50 =1.6 μM at 100 μM ATP). TBB also inhibits three other kinases with less potency: CDK2 (IC 50 =15.6 μM), phosphorylase kinase (IC 50 =8.7 μM) and glycogen synthase kinase 3β (GSK3β) (IC 50 =11.2 μM). All other kinases tested have IC50 values 50-fold greater than that for CK2. The viability of the androgen insensitive PC-3 cells may be diminished by TBB (60 μM TBB) acting either alone or combined with anticancer agents CPT or TRAIL when a proper time schedule of the administration is applied. The time schedule-dependent activity of TBB does not come from its effect on apoptosis in PC-3 cells. TBB is an ATP/GTP competitive inhibitor of protein kinase casein kinase-2 (CK2), has been examined against a panel of 33 protein kinases, either Ser/Thr- or Tyr-specific. In the presence of 10 μM TBB (and 100 μM ATP) only CK2 is drastically inhibited (>85%) whereas three kinases (phosphorylase kinase, glycogen synthase kinase 3L and cyclin-dependent kinase 2/cyclin A) underwent moderate inhibition, with IC 50 values one-two orders of magnitude higher than CK2 (IC 50 =0.9 μM). TBB also inhibits endogenous CK2 in cultured Jurkat cells. |
体内研究 | The extent of retinal neovascularization in a mouse OIR model is reduced by approximately 60% after treatment with TBB (6 days at 60 mg/kg per day). |
WGK Germany | 3 |
海关编号 | 29349990 |
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