TBB
Based on 15 publication(s) in Google Scholar
TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15 μM for rat liver CK2.
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- 純度: 98.54%
- CAS 番号: 17374-26-4
- 分子式: C6HBr4N3
- 分子量:434.71
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 TBB
More- Redox Biol. 2021 Oct;46:102098. [Abstract]
- Cell Death Dis. 2025 May 3;16(1):358. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- J Transl Med. 2022 Jul 21;20(1):325. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Biochem Pharmacol. 2018 Feb:148:41-51. [Abstract]
- J Virol. 2025 Dec 23;99(12):e0108925. [Abstract]
- Neurochem Res. 2024 May;49(5):1254-1267. [Abstract]
- Am J Pathol. 2024 Sep 5:S0002-9440(24)00331-6. [Abstract]
- J Cell Sci. 2024 May 1;137(9):jcs261241. [Abstract]
- Epigenetics Chromatin. 2023 Apr 19;16(1):11. [Abstract]
- J Mol Histol. 2023 Apr;54(2):135-145. [Abstract]
- Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287. [Abstract]
- Research Square Preprint. 2023 Dec 4.
- Tag der mündlichen Prüfung.14.07.2017
Customer Validation & Images
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生物活性
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-5-2 | CC50 |
>100 μM
Compound: TBBT
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Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay
Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay
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[PMID: 18625766] |
| Huh-5-2 | EC50 |
40 μM
Compound: TBBT
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Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay
Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay
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[PMID: 18625766] |
| Jurkat | DC50 |
17 μM
Compound: TBB
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Inhibition of cell viability in Jurkat T cells after 24 hrs by MTT method
Inhibition of cell viability in Jurkat T cells after 24 hrs by MTT method
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[PMID: 15566294] |
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. The time schedule-dependent activity of TBB does not come from its effect on apoptosis in PC-3 cells[2]. 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[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 17374-26-4
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性状 Solid
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分子量 434.71
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分子式 C6HBr4N3
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Color Off-white to yellow
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SMILES
BrC1=C2C(NN=N2)=C(Br)C(Br)=C1Br
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別名
NSC 231634; Casein Kinase II Inhibitor I
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (15)
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Journal Impact Factor
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Most Recent
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Redox Biol
Paeonol promotes Opa1-mediated mitochondrial fusion via activating the CK2α-Stat3 pathway in diabetic cardiomyopathy. [Abstract]2021 Oct;46:102098. PMID: 34418601 -
Cell Death Dis
TSPYL5-driven G3BP1 nuclear membrane translocation facilitates p53 cytoplasm sequestration via accelerating RanBP2-mediated p53 sumoylation and nuclear export in neuroblastoma. [Abstract]2025 May 3;16(1):358. PMID: 40319028 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
J Transl Med
NCAPG promotes the proliferation of hepatocellular carcinoma through the CKII-dependent regulation of PTEN. [Abstract]2022 Jul 21;20(1):325. PMID: 35864529 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Biochem Pharmacol
CK2α promotes advanced glycation end products-induced expressions of fibronectin and intercellular adhesion molecule-1 via activating MRTF-A in glomerular mesangial cells. [Abstract]2018 Feb:148:41-51. PMID: 29223351
TBB purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Feb:148:41-51. [Abstract]
Knockdown of CK2α expression with siRNA inhibits the expressions of fibronectin (FN) and intercellular adhesion molecule-1 (ICAM-1) in glomerular mesangial cells (GMCs)s induced by TBB (1 μM).
TBB purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Feb:148:41-51. [Abstract]
Inhibition of CK2α activity by TBB shows a similar effect, restrains the expression of myocardin-related transcription factor A (MRTF-A) in kidneys of diabetic mice.
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J Virol
The oncolytic avian reovirus p17 protein triggers chaperone-mediated autophagy by modulating Hsp90 and the T-complex protein-1 ring complex chaperones and co-chaperones to activate the IKK/NF-κB signaling. [Abstract]2025 Dec 23;99(12):e0108925. PMID: 41334925 -
Neurochem Res
Inhibition of CK2 Diminishes Fibrotic Scar Formation and Improves Outcomes After Ischemic Stroke via Reducing BRD4 Phosphorylation. [Abstract]2024 May;49(5):1254-1267. PMID: 38381246 -
Am J Pathol
Testosterone-Induced H3K27 Deacetylation Participates in Granulosa Cell Proliferation Suppression and Pathogenesis of Polycystic Ovary Syndrome. [Abstract]2024 Sep 5:S0002-9440(24)00331-6. PMID: 39243944 -
J Cell Sci
Tbl1 promotes Wnt/β-catenin signaling-induced degradation of the Tcf7l1 protein in mouse ESCs. [Abstract]2024 May 1;137(9):jcs261241. PMID: 38639717 -
Epigenetics Chromatin
Ovulatory signal-triggered chromatin remodeling in ovarian granulosa cells by HDAC2 phosphorylation activation-mediated histone deacetylation. [Abstract]2023 Apr 19;16(1):11. PMID: 37076890 -
J Mol Histol
C1orf109 promotes malignant phenotype of liver cancer via wnt signaling pathway in a CK2-dependent manner. [Abstract]2023 Apr;54(2):135-145. PMID: 36988773 -
Biochem Biophys Res Commun
β-catenin stimulates Tcf7l1 degradation through recruitment of casein kinase 2 in mouse embryonic stem cells. [Abstract]2020 Apr 2;524(2):280-287. PMID: 31987502
TBB purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287. [Abstract]
Western blot analysis of Tcf7l1 protein levels in mESCs pre-treated with the indicative different small molecules for 1 h and then treated with CHIR for 24 h.
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溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (230.04 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.75 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[4]
The heterozygous C57BL/6J mice are used. Emodin and TBB are injected intraperitoneally in volumes of 50 μL or less per mouse at doses of 15 to 30 mg/kg body weight, twice daily, starting from day 11. Control mice are injected with PEG-Tween vehicle alone.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (285 KB)
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- Korean - KR (393 KB)
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取扱説明書 (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[5]. Pagano MA, et al. The selectivity of inhibitors of protein kinase CK2: an update. Biochem J. 2008 Nov 1;415(3):353-65. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 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 | 0.2300 mL | 1.1502 mL | 2.3004 mL | 5.7510 mL | |
| 15 mM | 0.1534 mL | 0.7668 mL | 1.5336 mL | 3.8340 mL | |
| 20 mM | 0.1150 mL | 0.5751 mL | 1.1502 mL | 2.8755 mL | |
| 25 mM | 0.0920 mL | 0.4601 mL | 0.9202 mL | 2.3004 mL | |
| 30 mM | 0.0767 mL | 0.3834 mL | 0.7668 mL | 1.9170 mL | |
| 40 mM | 0.0575 mL | 0.2875 mL | 0.5751 mL | 1.4377 mL | |
| 50 mM | 0.0460 mL | 0.2300 mL | 0.4601 mL | 1.1502 mL | |
| 60 mM | 0.0383 mL | 0.1917 mL | 0.3834 mL | 0.9585 mL | |
| 80 mM | 0.0288 mL | 0.1438 mL | 0.2875 mL | 0.7189 mL | |
| 100 mM | 0.0230 mL | 0.1150 mL | 0.2300 mL | 0.5751 mL |
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