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TBB

产品编号 T2695 CAS 17374-26-4

别名: Casein Kinase II Inhibitor I, NSC 231634, 4,5,6,7-tetrabromobenzotriazole

TBB (NSC-231634) 是一种高选择性的 ATP/GTP 竞争性酪蛋白激酶 2 (CK2) 抑制剂，可抑制大鼠肝脏 CK2，IC50值为0.15 μM。

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TBB, CAS 17374-26-4

规格	价格/CNY	货期
5 mg	￥ 279	现货
10 mg	￥ 393	现货
25 mg	￥ 659	现货
50 mg	￥ 979	现货
100 mg	￥ 1,470	现货
200 mg	￥ 2,270	现货
1 mL * 10 mM (in DMSO)	￥ 298	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	TBB (NSC-231634)(NSC-231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2).
靶点活性	CK2:0.4 μM(Ki), CK1:47 μM(Ki)
体外活性	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=1.6 μM at 100 μM ATP). TBB also inhibits three other kinases with less potency: CDK2 (IC50=15.6 μM), phosphorylase kinase (IC50=8.7 μM) and glycogen synthase kinase 3β (GSK3β) (IC50=11.2 μM). All other kinases tested have IC50 values 50-fold greater than that for CK2[1]. 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. However, the time schedule-dependent activity of TBB does not come from its effect on apoptosis in PC-3 cells[2]. It is because that TBB is an ATP/GTP competitive inhibitor of protein kinase casein kinase-2 (CK2) which 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 IC50 values one-two orders of magnitude higher than CK2 (IC50=0.9 μM). TBB also inhibits endogenous CK2 in cultured Jurkat cells[3].
体内活性	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) which is the most specific CK2 inhibitor known[4].
激酶实验	Kinase assay: Total kinase activity of CaMKII, determined in a standard 2 min assay (100 μL), contained 35 mM HEPES, 10 mM MgCl2, 1 mM CaCl2, 10 μg of chicken gizzard myosin 20-kD light chain, 0.1 μM calmodulin, and 10 μM [γ-33]ATP at 30 °C. The kinase reaction is halted by adding 1 mL of 10% trichloroacetic acid.
细胞实验	TBB is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. 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 (100 μg/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 60 μM), CPT (final concentration 5.8 nM), 2-deoxyglucose (2-DG; final concentration 0.5 mM) or TRAIL (final concentration 13.3 ng/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 500 μL of MTT mixture (0.5 mg/mL for PC-3 and 5.0 mg/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 250 μL of DMSO. The absorbance is measured at 570 nm[2].

别名	Casein Kinase II Inhibitor I, NSC 231634, 4,5,6,7-tetrabromobenzotriazole
分子量	434.71
分子式	C6HBr4N3
CAS No.	17374-26-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 43.5 mg/mL(100 mM)

Ethanol: 100 mM

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	2.3004 mL	11.5019 mL	23.0038 mL	57.5096 mL
	5 mM	0.4601 mL	2.3004 mL	4.6008 mL	11.5019 mL
	10 mM	0.23 mL	1.1502 mL	2.3004 mL	5.751 mL
	20 mM	0.115 mL	0.5751 mL	1.1502 mL	2.8755 mL
	50 mM	0.046 mL	0.23 mL	0.4601 mL	1.1502 mL
	100 mM	0.023 mL	0.115 mL	0.23 mL	0.5751 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

1. De Moliner E, et al. Alternative binding modes of an inhibitor to two different kinases. Eur J Biochem. 2003 Aug;270(15):3174-81. 2. Orzechowska E, et al. Time schedule-dependent effect of the CK2 inhibitor TBB on PC-3 human prostate cancer cell viability. Oncol Rep. 2012 Jan;27(1):281-5. 3. Sarno S, et al. Selectivity of 4,5,6,7-tetrabromobenzotriazole, an ATP site-directed inhibitor of protein kinase CK2 ('casein kinase-2'). FEBS Lett. 2001 May 4;496(1):44-8. 4. Ljubimov AV, et al. Involvement of protein kinase CK2 in angiogenesis and retinal neovascularization. Invest Ophthalmol Vis Sci. 2004 Dec;45(12):4583-91. 5. Wang C, De Su L, Shao Y M, et al. Involvement of PML-I in reformation of PML nuclear bodies in acute promyelocytic leukemia cells by leptomycin B[J]. Toxicology and applied pharmacology. 2019, 384: 114775. 6. Zhu S, Cheng X, Wang R, et al. Restoration of microRNA function impairs MYC-dependent maintenance of MLL leukemia[J]. Leukemia. 2020: 1-5.

文献引用

1. Zhu S, Cheng X, Wang R, et al. Restoration of microRNA function impairs MYC-dependent maintenance of MLL leukemia. Leukemia. 2020: 1-5 2. Wang C, De Su L, Shao Y M, et al. Involvement of PML-I in reformation of PML nuclear bodies in acute promyelocytic leukemia cells by leptomycin B. Toxicology and Applied Pharmacology. 2019, 384: 114775

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

TBB 17374-26-4 Cell Cycle/Checkpoint Metabolism PI3K/Akt/mTOR signaling Stem Cells Casein Kinase GSK-3 CDK inhibit Casein Kinase II Inhibitor I NSC-231634 Inhibitor NSC231634 NSC 231634 4,5,6,7-tetrabromobenzotriazole inhibitor

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TBB

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

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剂量换算

体内实验配液计算器

技术支持

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