17374-26-4
基本信息
4,5,6,7-四溴苯并三唑
4,5,6,7-四溴苯基三唑
4,5,6,7-四溴-1H-苯并三唑
TBB(4,5,6,7-四溴-1H-苯并三唑)
TBBT
NSC 231634
CK2 INHIBITOR
TBB(NSC 231634)
TBB (enzyMe inhibitor)
4,5,6,7-Tetrabromotriazole
CASEIN KINASE II INHIBITOR I
4,5,6,7-TETRABROMOBENZOTRIAZOLE
CASEIN KINASE II INHIBITOR *TBB**
物理化学性质
| 熔点 | 262-266°C |
| 沸点 | 552.5±45.0 °C(Predicted) |
| 密度 | 2.840±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 储存条件 | 2-8°C |
| 溶解度 | DMSO: 28 mg/mL |
| 溶解度 | 在DMSO中的溶解度为28 毫克/毫升 |
| 酸度系数(pKa) | 3.87±0.40(Predicted) |
| 形态 | solid |
| 颜色 | white |
| 最大波长(λmax) | 300nm(MeOH)(lit.) |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P305+P351+P338 |
| WGK Germany | 3 |
| WGK Germany | 3 |
| 海关编码 | 29349990 |
常见问题列表
|
CK2 0.15 μM (IC 50 , Human CK2) |
PIM1 1.04 μM (IC 50 ) |
PIM2 4.3 μM (IC 50 ) |
PIM3 0.86 μM (IC 50 ) |
HIPK2 5.3 μM (IC 50 ) |
HIPK3 4.9 μM (IC 50 ) |
DYRK1a 4.36 μM (IC 50 ) |
DYRK2 0.99 μM (IC 50 ) |
DYRK3 5.3 μM (IC 50 ) |
PKD1 5.9 μM (IC 50 ) |
CDK2 14 μM (IC 50 ) |
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.
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).