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TBB

酪蛋白激酶-2（CK2）抑制剂，TBB是可渗透细胞，ATP竞争型的 CK2 抑制剂，抑制大鼠肝脏CK2的 IC50 值为0.15 μM。

目录号: PC15444 纯度: ≥98%

CAS No. :17374-26-4

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中文名称

TBB

中文别名

TBB(4,5,6,7-四溴-1H-苯并三唑);4,5,6,7-四溴苯基三唑;4,5,6,7-四溴苯并三唑;3,5-二(4-硝基苯氧基)苯甲酸;4,5,6,7-Tetrabromobenzotriazole 4,5,6,7-四溴苯并三唑;4,5,6,7-四溴-1H-苯并三唑;4,5,6,7-四溴苯甲腈;野黄芩素, 来源于半枝莲;7-四溴苯并三唑;4,5,6,7-四溴苯并三唑, 选择性细胞渗透性酪蛋白激酶2(CK2)抑制剂

英文名称

TBB

英文别名

4,5,6,7-Tetrabromo-1H-benzo[d][1,2,3]triazole;TBB;1H-Benzotriazole, 4,5,6,7-tetrabromo-;4,5,6,7-Tetrabromo-1;4,5,6,7-Tetrabromo-1H-benzotriazole;4,5,6,7-TETRABROMOBENZOTRIAZOLE;4,5,6,7-Tetrabromo-2-azabenzimidazole 4,5,6,7-Tetrabromobenzotriazole;4,5,6,7-tetrabromo-2H-benzotriazole;NSC 231634;TBB (enzyme inhibitor);4,5,6,7-Tetrabromo-2-azabenzimidazole;TBBt;CK2 INHIBITOR;TBB(NSC 231634);4,5,6,7-Tetrabromotriazole;CASEIN KINASE II INHIBITOR I;CASEIN KINASE II INHIBITOR *TBB**;TETRABROMO-2-BENZOTRIAZOLE;NSC231634;InSolution™ Casein Kinase II Inhibitor I;TBB;TBBT;1p5e;C6HBr4N3;GTPL9372;STO170;BDBM11323

Cas No.

17374-26-4

分子式

C₆N₃Br₄H

分子量

434.71

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC₅₀ of 0.15 μM for rat liver CK2.

性状

Solid

IC50 & Target[1][2]

CK2

0.15 μM (IC₅₀, Human CK2)

PIM1

1.04 μM (IC₅₀)

PIM2

4.3 μM (IC₅₀)

PIM3

0.86 μM (IC₅₀)

HIPK2

5.3 μM (IC₅₀)

HIPK3

4.9 μM (IC₅₀)

DYRK1a

4.36 μM (IC₅₀)

DYRK2

0.99 μM (IC₅₀)

DYRK3

5.3 μM (IC₅₀)

PKD1

5.9 μM (IC₅₀)

CDK2

14 μM (IC₅₀)

体外研究(In Vitro)

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. 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. 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 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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. [Information]

[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. [Information]

[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. [Information]

[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. [Information]

[5]. Pagano MA, et al. The selectivity of inhibitors of protein kinase CK2: an update. Biochem J. 2008 Nov 1;415(3):353-65. [Information]

[6]. Chen Z, et al. CK2α promotes advanced glycation end products-induced expressions of fibronectin and intercellular adhesion molecule-1 via activating MRTF-A in glomerular mesangial cells. Biochem Pharmacol. 2017 Dec 6;148:41-51. [Information]

溶解度数据

体外研究:

DMSO : ≥ 100 mg/mL (230.04 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3004 mL	11.5019 mL	23.0038 mL
5 mM	0.4601 mL	2.3004 mL	4.6008 mL
10 mM	0.2300 mL	1.1502 mL	2.3004 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.75 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (5.75 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.75 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.75 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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