Home Immunology & Inflammation TBK1 inhibitor GSK8612 For research use only.

GSK8612

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 GSK8612 could be identified.

GSK8612 Chemical Structure

GSK8612 Chemical Structure

CAS No. 2361659-62-1

Purity & Quality Control

GSK8612 Related Products

Biological Activity

Description 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 GSK8612 could be identified.
Targets
TBK1 [1]
6.8(pIC50)
In vitro
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, GSK8612 is able to inhibit secretion of interferon beta (IFNβ) in response to dsDNA and cGAMP, the natural ligand for STING. GSK8612 has lower affinity for phosphorylated TBK1. GSK8612 inhibits recombinant TBK1 with an average pIC50 of 6.8 in a biochemical functional assay. The actual selectivity of GSK8612 for TBK1 in the cells will depend on the activation state of TBK1[1].
Cell Research Cell lines Ramos cells
Concentrations 6.8 (pKd)
Incubation Time 1 h
Method

Ramos cells were exposed to GSK8612 for 60 min in cell culture media (RPMI1640, Gibco) containing 2% fetal bovine serum (FBS, Gibco) and then stimulated with poly(I:C) (30 µg/mL, Invivogen) for 120 min at 37°C, 5% CO2.
In Vivo
In vivo

GSK8612 is highly protein bound in mouse, rat and human blood[1].
Animal Research Animal Models Male BALB/c nude and C57BL/6 mice
Dosages 5 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 520.33 Formula

C17H17BrF3N7O2S
CAS No. 2361659-62-1 SDF --
Smiles CC1=NN(C=C1NC2=NC=C(C(=N2)NCC3=CC=C(C=C3)S(=O)(=O)N)Br)CC(F)(F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (192.18 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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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.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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