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GSK8612 TBK1 inhibitor

Name: GSK8612
Brand: Selleck Chemicals
SKU: S8872
Availability: InStock
Rating: 5 (25 reviews)

Cat.No.S8872

GSK8612 is a highly potent and selective inhibitor for TBK1 (Tank-binding Kinase-1) with pKd of 8.0. Within 10-fold affinity with respect to TBK1, no off-targets of this compound could be identified.

Chemical Structure

Molecular Weight: 520.33

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Quality Control

Batch: Purity: 99.86%

99.86

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Other TBK1 Inhibitors	MRT67307

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (192.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

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.
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.	12.500mg/ml (24.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 250 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.

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	520.33	Formula	C₁₇H₁₇BrF₃N₇O₂S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2361659-62-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=NN(C=C1NC2=NC=C(C(=N2)NCC3=CC=C(C=C3)S(=O)(=O)N)Br)CC(F)(F)F

Mechanism of Action

Targets/IC₅₀/Ki	TBK1 6.8(pIC50)
In vitro	In cellular assays, this small molecule inhibits toll-like receptor (TLR)3-induced interferon regulatory factor (IRF)3 phosphorylation in Ramos cells and type I interferon (IFN) secretion in primary human mononuclear cells. In THP1 cells, this compound is able to inhibit secretion of interferon beta (IFNβ) in response to dsDNA and cGAMP, the natural ligand for STING. It has lower affinity for phosphorylated TBK1. This chemical inhibits recombinant TBK1 with an average pIC50 of 6.8 in a biochemical functional assay. The actual selectivity of this compound for TBK1 in the cells will depend on the activation state of TBK1.
In vivo	This compound is highly protein bound in mouse, rat and human blood.
References	[1] https://pubmed.ncbi.nlm.nih.gov/31097999/ [2] https://pubmed.ncbi.nlm.nih.gov/33679751/

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Handling Instructions

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