TBB  ≥98%

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包装规格:10mg 50mg 250mg 1g 5g in glass bottle
溶解性:溶于DMSO(≥ 100 mg/mL)
产品描述:基本信息 产品编号:T10774 产品名称:TBB CAS: 17374-26-4   储存条件 粉末 2-8℃ 四年     分子式: C6HBr4N3 溶于液体 -80℃ 两年 分子量 434.71 -20℃ 一个月 化学名:  4,5,6,7-Tetrabromo-2-azabenzimidazole   Solubility (25°C)   体外 DMSO 86 mg/mL (197.83mM) Ethanol   Water   体内 现配现用   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3004mL 11.5019mL 23.0038mL 5mM 0.4601mL 2.3004mL 4.6008mL 10mM 0.2300mL 1.1502mL 2.3004mL 50mM 0.0460mL 0.2300mL 0.4601mL   生物活性 产品描述 一种可渗透细胞,ATP竞争型的 CK2 抑制剂。 靶点/IC50 CK2 (Cell-free assay) 0.4μM(Ki) CK1 (Cel-free assay) 47μM(Ki) 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: IC50=1.6μM at 100μM ATP). TBB also inhibits three other kinases with less potency: CDK2 (IC50=15.6μM), phosphorylase kinase (IC50=8.7μM) and glycogen synthase kinase 3β (GSK3β) (IC50=11.2μM). 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 (60μM 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 100μM 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 IC50 values one-two orders of magnitude higher than CK2 (IC50=0.9μM). 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).   推荐实验方法(仅供参考) 细胞实验: Cell Assay PC-3 or HeLa cells are cultured routinely in RPMI-1640 and DMEM media, respectively, which are supplemented with 10% FBS, Penicillin (100 U/mL) and Streptomycin (100μg/mL) at 37°C in a humidified atmosphere of 5% CO2. Cells are seeded at 5×104  cells/well (PC-3) or 2×104 (HeLa) in 24-wells plates and cultured for 72 h. TBB (final concentration 60μM), CPT (final concentration 5.8nM), 2-deoxyglucose (2-DG; final concentration 0.5mM) or TRAIL (final concentration 13.3ng/mL) are added to the medium individually or in a combination and the cells are cultured for additional time, indicated on each figure. After treatment, the medium with the agent is removed and 500μL of MTT mixture (0.5mg/mL for PC-3 and 5.0mg/mL for HeLa cells in medium without phenol red) is added to each well and incubated for an additional 1 h at 37°C. The formazan crystals are diluted in 250μL of DMSO. The absorbance is measured at 570nm.   动物实验:   Animal Administration Mice The heterozygous C57BL/6J mice are used. Emodin and TBB are injected intraperitoneally in volumes of 50μL or less per mouse at doses of 15 to 30mg/kg body weight, twice daily, starting from day 11. Control mice are injected with PEG-Tween vehicle alone.
保存条件:2-8℃