4,5,6,7-四溴-1H-苯并三唑
- CAS号:17374-26-4
- 英文名:4,5,6,7-TETRABROMOBENZOTRIAZOLE
- 中文名:4,5,6,7-四溴-1H-苯并三唑
- CBNumber:CB9104424
- 分子式:C6HBr4N3
- 分子量:434.71
- MOL File: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
- 形态 :solid
- 酸度系数(pKa) :3.87±0.40(Predicted)
- 颜色 :white
- 最大波长(λmax) :300nm(MeOH)(lit.)
- WGK Germany :3
- 海关编码 :29349990
4,5,6,7-四溴-1H-苯并三唑性质、用途与生产工艺
- 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 )
-
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).
- 更新日期:2024/11/08
- 产品编号:HY-14394
- 产品名称:TBB
- CAS编号:
- 包装:5 mg
- 价格:300元
- 更新日期:2024/11/08
- 产品编号:HY-14394
- 产品名称:4,5,6,7-四溴-1H-苯并三唑 TBB
- CAS编号:17374-26-4
- 包装:10mM * 1mLin DMSO
- 价格:330元
- 公司名称:Labinova AB
- 联系电话:--
- 电子邮件:info@labinova.se
- 国家:欧洲
- 产品数:281
- 优势度:64