生物活性

TBB is a cell-permeable, selective inhibitor of casein kinase-2 (CK2) (IC50 = 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively). Exhibits modest discrimination between CK2 subunits, with Ki values ranging from 80 nM to 210 nM. Acts in an ATP/GTP-competitive manner and displays one to two orders of magnitude selectivity over a panel of 33 protein kinases.

体外研究

体内研究

激酶实验

细胞实验

动物实验

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Sarno, S., et al., 2001. Selectivity of 4,5,6,7-tetrabromobenzotriazole, an ATP site-directed inhibitor of protein kinase CK2 ('casein kinase-2'). FEBS letters. 496(1): 44-8. PMID: 11343704
[2] Borowski, Peter., et al., 2003. Halogenated benzimidazoles and benzotriazoles as inhibitors of the NTPase/helicase activities of hepatitis C and related viruses. European journal of biochemistry / FEBS. 270(8): 1645-53. PMID: 12694177
[3] Sarno, Stefania., et al., 2003. Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA). The Biochemical journal. 374(Pt 3): 639-46. PMID: 12816539
[4] Duncan, James S., et al., 2008. An unbiased evaluation of CK2 inhibitors by chemoproteomics: characterization of inhibitor effects on CK2 and identification of novel inhibitor targets. Molecular & cellular proteomics : MCP. 7(6): 1077-88. PMID: 18258654
[5] Fromageot, H P., et al., 1977. Adsorption of human erythrocyte surface glycoprotein onto polystyrene latex spheres. The Journal of laboratory and clinical medicine. 90(2): 324-9. PMID: 886218
[6] Ruzzene, Maria., et al., 2002. Protein kinase CK2 inhibitor 4,5,6,7-tetrabromobenzotriazole (TBB) induces apoptosis and caspase-dependent degradation of haematopoietic lineage cell-specific protein 1 (HS1) in Jurkat cells. The Biochemical journal. 364(Pt 1): 41-7. PMID: 11988074

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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