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TBB Casein Kinase inhibitor

Name: TBB
Brand: Selleck Chemicals
SKU: S5265
Availability: InStock
Rating: 5 (12 reviews)

Cat.No.S5265

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.

Chemical Structure

Molecular Weight: 434.71

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Quality Control

Batch: S526501 DMSO]86 mg/mL]false]]]false]]]false Purity: 99.68%

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.68

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other Casein Kinase Inhibitors	Silmitasertib (CX-4945) Silmitasertib (CX-4945) sodium salt D 4476 IC261 PF-670462 (E/Z)-GO289 TTP 22 Longdaysin PF 4800567 5,6-Dichlorobenzimidazole 1-beta-D-ribofuranoside

Solubility

In vitro
Batch:

DMSO : 86 mg/mL (197.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.150mg/ml (4.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 43 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.350mg/ml (0.81mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	434.71	Formula	C₆HBr₄N₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	17374-26-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	4,5,6,7-tetrabromobenzotriazole			Smiles	C1(=C(C2=NNN=C2C(=C1Br)Br)Br)Br

Mechanism of Action

Targets/IC₅₀/Ki	CK2 (Cell-free assay) 0.4 μM(Ki) CK1 (Cel-free assay) 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). This compound discriminates between CK2 and CK1, being much more e¡ective with the former.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11343704/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02812290	Recruiting	Lung Transplant Rejection	University of Alberta	May 2016	--
NCT02235779	Unknown status	Interstitial Lung Disease	Laval University	August 2014	Not Applicable
NCT00888212	Completed	Sarcoidosis	University Hospital Ghent	June 2008	Not Applicable

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