CAS NO: | 577779-57-8 |
包装 | 价格(元) |
25mg | 电议 |
250mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 433.7 |
Cas No. | 577779-57-8 |
Formula | C7H2Br4N2 |
Synonyms | Casein Kinase II Inhibitor XII,TBBz |
Solubility | Soluble in DMSO |
Chemical Name | 4,5,6,7-tetrabromo-1H-benzimidazole |
Canonical SMILES | BrC1=C2C(N=CN2)=C(Br)C(Br)=C1Br |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Ki: 0.5-1 μM
4,5,6,7-Tetrabromobenzimidazole is a CK2 inhibitor.
Casein kinase 2 (CK2), a constitutive protein kinase involved in many signal transduction pathways, is known to be able to negatively regulate apoptosis, and its activity is increased in various proliferating tissues and tumors.
In vitro: Previous study found that like the reported 4,5,6,7-tetrabromobenzotriazole (TBBt), the structurally related 4,5,6,7-tetrabromobenzimidazole (TBBz) was a selective ATP-competitive inhibitor of protein kinase CK2 from various sources including yeast, rat liver, Neurospora crassa and Candida tropicalis, with K(i) values in the range 0.5-1 μM. TBBz was found to virtually inactive vs. PKA, PKC, and a very weak inhibitor of protein kinase CK1. TBBt was noted to be a more effective inhibitor of PK60S than of yeast CK2; by contrast, TBBz was a relatively feeble inhibitor of PK60S, thus more selective than TBBt vs. CK2 in yeast cells. Therefore, similar to TBBt, TBBz could be regarded as an additional lead compound for development of more potent inhibitors of CK2 [1].
In vivo: Up to now, therer is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Zien, P. ,Bretner, M.,Zastapilo, K., et al. Selectivity of 4,5,6,7-tetrabromobenzimidazole as an ATP-competitive potent inhibitor of protein kinase CK2 from various sources. Biochemical and Biophysical Research Communications 306(1), 129-133 (2003).