产品介绍 |
TBB(NSC 231634)是ATP/GTP竞争性CK2抑制剂,对鼠肝和人重组CK2的IC50分别为0.9和1.6 μM。 |
别名 |
4,5,6,7-四溴苯并三唑;NSC 231634; TBB (enzyme inhibitor);1H-Benzotriazole;4,5,6,7-Tetrabromobenzotriazole; 4,5,6,7-Tetrabromo-2-azabenzimidazole; TBBt |
生化机理 |
TBB is a cell-permeable benzotriazolo compound that acts as a highly selective ATP/GTP-competitive protein kinase inhibitor. It has been shown to specifically inhibit casein kinase IIα (CK2α) and dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A (Dyrk1A). TBB’s strong binding action appears to result from both hydrophobic and van der Walls interactions. Other kinases such as GSK (glycogen synthase kinase), Cdk2 (CDK2) and phosphorylase kinase were inhibited to a lesser extent. TBB has also been shown to inhibit NS3-associated viral helicase activities in hepatitis C virus and West Nile virus. TBB has been used as an apoptotic inducer in Jerkat cells. |
应用 |
A highly selective CK2α, Dyrk1A, and NS3 viral helicase inhibitor. |