TBB

Catalog No.S5265 Batch:S526501

Technical Data

Formula	C₆HBr₄N₃
Molecular Weight	434.71	CAS No.	17374-26-4
Solubility (25°C)*	In vitro	DMSO	86 mg/mL (197.83 mM)


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

TBB (4,5,6,7-tetrabromobenzotriazole) is a selective cell-permeable CK2 inhibitor with IC50 values of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively.

Targets

CK2 ^[1] (Cell-free assay)	CK1 ^[1] (Cel-free assay)
0.4 μM(Ki)	47 μM(Ki)

In vitro

In the presence of 10 μM TBB (and 100 μM ATP) only CK2 was drastically inhibited (s85%) 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 discriminates between CK2 and CK1, being much more e¡ective with the former^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Jurkat cells Concentrations 60 μM Incubation Time 2 h Method Cell treatment was performed by incubation of cell suspension (~10×10⁶ cells/ml) for 2 h at 37℃ in the presence of 2 μM okadaic acid (OA) with the addition of protein kinase inhibitors where indicated. After incubations, cells were centrifuged and lysed for 15 min in ice-cold buffer consisting of 20 mM Tris^HCl pH 7.4, 2 mM EDTA, 2 mM EGTA, 10 mM 2-mercaptoethanol, 10% (v/v) glycerol, 1 mM Na3VO4, 0.05% Nonidet P-40, protease inhibitor cocktail, 10 mM NaF, 1 μM OA. The lysate was cleared by centrifugation for 10 min at 14 000 rpm.

Cell Assay:^{^[1]}

Cell lines
Jurkat cells
Concentrations
60 μM
Incubation Time
2 h
Method
Cell treatment was performed by incubation of cell suspension (~10×10⁶ cells/ml) for 2 h at 37℃ in the presence of 2 μM okadaic acid (OA) with the addition of protein kinase inhibitors where indicated. After incubations, cells were centrifuged and lysed for 15 min in ice-cold buffer consisting of 20 mM Tris^HCl pH 7.4, 2 mM EDTA, 2 mM EGTA, 10 mM 2-mercaptoethanol, 10% (v/v) glycerol, 1 mM Na3VO4, 0.05% Nonidet P-40, protease inhibitor cocktail, 10 mM NaF, 1 μM OA. The lysate was cleared by centrifugation for 10 min at 14 000 rpm.

References

[1] Sarno S, et al. FEBS Lett. 2001, 496(1):44-8.

Selleck's TBB has been cited by 12 publications

The ARID1A-METTL3-m6A axis ensures effective RNase H1-mediated resolution of R-loops and genome stability [ Cell Rep, 2024, 43(2):113779]	PubMed: 38358891
Genome-scale mapping of DNA damage suppressors through phenotypic CRISPR-Cas9 screens [ Mol Cell, 2023, 83(15):2792-2809.e9]	PubMed: 37478847
CK2-Mediated Phosphorylation Upregulates the Stability of USP13 and Promotes Ovarian Cancer Cell Proliferation [ Cancers (Basel), 2022, 15(1)200]	PubMed: 36612196
Unphosphorylated Form of the PAQosome Core Subunit RPAP3 Binds Ribosomal Preassembly Complexes to Modulate Ribosome Biogenesis [ J Proteome Res, 2022, 21(4):1073-1082]	PubMed: 35129352
CK2-mediated phosphorylation of Che-1/AATF is required for its pro-proliferative activity [ J Exp Clin Cancer Res, 2021, 40(1):232]	PubMed: 34266450
The catalytic subunit of Plasmodium falciparum casein kinase 2 is essential for gametocytogenesis [ Commun Biol, 2021, 4(1):336]	PubMed: 33712726
Development of a Cell-Based Luciferase Complementation Assay for Identification of SARS-CoV-2 3CLpro Inhibitors [ Viruses, 2021, 13(2)173]	PubMed: 33498923
The unphosphorylated form of the PAQosome core subunit RPAP3 binds ribosomal preassembly complexes to modulate ribosome biogenesis [ bioRxiv, 2021, 10.1101/2021.03.17.435124]	PubMed: None
GLP-catalyzed H4K16me1 promotes 53BP1 recruitment to permit DNA damage repair and cell survival. [ Nucleic Acids Res, 2019, 47(21):10977-10993]	PubMed: 31612207
Protein Kinase CK2 Subunits Differentially Perturb the Adhesion and Migration of GN11 Cells: A Model of Immature Migrating Neurons [ Int J Mol Sci, 2019, 20(23)E5951]	PubMed: 31779225

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.