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 |
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中文同义词 | 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;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 |
英文名称 | 4,5,6,7-TETRABROMOBENZOTRIAZOLE |
英文同义词 | NSC 231634;TBB;TBBT;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;1H-Benzotriazole, 4,5,6,7-tetrabroMo-;TBB (enzyMe inhibitor) |
CAS号 | 17374-26-4 |
分子式 | C6HBr4N3 |
分子量 | 434.71 |
EINECS号 | |
相关类别 | 小分子抑制剂;小分子抑制剂,天然产物;细胞生物学试剂;Akt;mTOR;Protein Kinase Inhibitors and Activators;Protein Kinase;PI3K/Akt/mTOR;Inhibitors;PI3K |
Mol文件 | 17374-26-4.mol |
结构式 |
4,5,6,7-四溴-1H-苯并三唑 性质
熔点 | 262-266°C |
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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 | 在DMSO中的溶解度为28 毫克/毫升 |
形态 | 固体 |
酸度系数(pKa) | 3.87±0.40(Predicted) |
颜色 | 白色 |
最大波长(λmax) | 300nm(MeOH)(lit.) |
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).
安全信息
WGK Germany | 3 |
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海关编码 | 29349990 |
提供商 | 语言 |
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英文
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-14394 | TBB | 5 mg | 300元 | |
2024/08/19 | HY-14394 | 4,5,6,7-四溴-1H-苯并三唑 TBB | 17374-26-4 | 10mM * 1mLin DMSO | 330元 |