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| 25mg |
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Purity: ≥98%
TBB (NSC 231634; Casein Kinase II Inhibitor I) is a novel, potent, cell-permeable and ATP-competitive inhibitor of protein kinase CK2 with an IC50 of 0.15 μM for rat liver CK2. TBB induces apoptosis and caspase-dependent degradation of haematopoietic lineage cell-specific protein 1 (HS1) in Jurkat cells. Inhibitors of CK2 kinase inhibit cell proliferation and induce apoptosis in numerous cancer cell lines. Due to these properties, they are considered potentially useful in anticancer therapy. I
| ln Vitro |
Casein kinase 2, or CK2, has the highest inhibitory capacity of TBB, according to studies employing a panel of 33 protein kinases (human CK2: IC50=1.6 μM at 100 μM ATP). Additionally, three less powerful kinases are inhibited by TBB: glycogen synthase kinase 3β (GSK3β) (IC50=11.2 μM), phosphorylase kinase (IC50=8.7 μM), and CDK2 (IC50=15.6 μM). Compared to CK2, the IC50 values of all other examined kinases were 50 times higher [1]. When administered according to the recommended dosage schedule, TBB (60 μM TBB) either by itself or in conjunction with the anticancer drugs CPT or TRAIL may decrease the viability of androgen-insensitive PC-3 cells. TBB's effect on PC-3 cell apoptosis is not the cause of its time-dependent activity [2]. Tested against 33 protein kinases (Ser/Thr-specific or Tyr-specific), TBB is an ATP/GTP competitive inhibitor of the protein kinase casein kinase 2 (CK2). While three kinases (phosphorylase kinase, glycogen synthase kinase 3L, and cyclin-dependent kinase 2/ Cyclin A) were moderately inhibited, with an IC50 value one to two orders of magnitude higher than CK2 (IC50=0.9 μM), only CK2 was significantly inhibited (>85%) in the presence of 10 μM TBB (and 100 μM ATP). Additionally, in cultivated Jurkat cells, TBB suppresses endogenous CK2 [3].
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| ln Vivo |
In the mouse OIR model, the degree of retinal neovascularization was reduced by about 60% following treatment with TBB (60 mg/kg per day for 6 days) [4].
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| References |
[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]. Pagano MA, et al. The selectivity of inhibitors of protein kinase CK2: an update. Biochem J. 2008 Nov 1;415(3):353-65. [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 |
| Molecular Formula |
C6HBR4N3
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|---|---|
| Molecular Weight |
434.7082
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| CAS # |
17374-26-4
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| SMILES |
BrC1=C(NN=N2)C2=C(Br)C(Br)=C1Br
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| InChi Key |
OMZYUVOATZSGJY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6HBr4N3/c7-1-2(8)4(10)6-5(3(1)9)11-13-12-6/h(H,11,12,13)
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| Chemical Name |
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole
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| Synonyms |
Casein Kinase II Inhibitor I, Tetrabromobenzotriazole, NSC 231634, NSC231634, NSC-231634
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~230.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.75 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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