4,5,6,7-四溴-1H-苯并三唑
中文名称:
4,5,6,7-四溴-1H-苯并三唑
中文同义词:
7-四溴-1H-苯并三唑;蛋白激酶CK2抑制剂(TBB);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;4,5,6,7-四溴苯并三唑;7-四溴苯并三唑;4,5,6,7-四溴苯基三唑;TBB(4,5,6,7-四溴-1H-苯并三唑);4,5,6,7-四溴-1H-苯并三唑
英文名称:
4,5,6,7-TETRABROMOBENZOTRIAZOLE
英文同义词:
NSC 231634;TBB;TBBT;7-tetrabromo-;NSC 231634; TBB (ENZYME INHIBITOR);1H-BENZOTRIAZOLE; 4;5;6;7-TETRABROMO-;4,5,6,7-Tetrabromo-1H-benzotriazole;CASEIN KINASE II INHIBITOR *TBB**;4,5,6,7-Tetrabromo-2-azabenzimidazole, 4,5,6,7-Tetrabromobenzotriazole, NSC 231634, TBBt
CAS号:
17374-26-4
分子式:
C6HBr4N3
分子量:
434.71
EINECS号:
相关类别:
细胞生物学试剂;小分子抑制剂;小分子抑制剂，天然产物;Akt;mTOR;PI3K;Inhibitors;Protein Kinase Inhibitors and Activators;Protein Kinase;PI3K/Akt/mTOR
Mol文件:
17374-26-4.mol
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
溶解度
DMSO: 28 mg/mL
酸度系数(pKa)
3.87±0.40(Predicted)
形态
solid
颜色
white
最大波长(λmax)
300nm(MeOH)(lit.)
生物活性
TBB是可渗透细胞，ATP竞争型的 CK2 抑制剂，抑制大鼠肝脏CK2的 IC50 值为0.15 μM。
靶点
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 )
CK2
0.15 μM (IC 50 , Human CK2)
PIM1
1.04 μM (IC 50 )
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
海关编码
29349990
