GSK8612

Catalog No.S8872 Batch:S887202

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Technical Data

Formula

C17H17BrF3N7O2S
Molecular Weight 520.33 CAS No. 2361659-62-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (192.18 mM)
Ethanol 2 mg/mL (3.84 mM)
Water Insoluble
* <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 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 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].
In vivo

GSK8612 is highly protein bound in mouse, rat and human blood[1].

Protocol (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[2]
  • Animal Models

    Male BALB/c nude and C57BL/6 mice

  • Dosages

    5 mg/kg

  • Administration

    p.o.

Selleck's GSK8612 has been cited by 16 publications

AKT and EZH2 inhibitors kill TNBCs by hijacking mechanisms of involution [ Nature, 2024, 10.1038/s41586-024-08031-6] PubMed: 39385030
TBK1-Zyxin signaling controls tumor-associated macrophage recruitment to mitigate antitumor immunity [ EMBO J, 2024, 10.1038/s44318-024-00244-9] PubMed: 39304793
A TLR4/TRAF6-dependent signaling pathway mediates NCoR coactivator complex formation for inflammatory gene activation [ Proc Natl Acad Sci U S A, 2024, 121(2):e2316104121] PubMed: 38165941
Galectin-9 blockade synergizes with ATM inhibition to induce potent anti-tumor immunity [ Int J Biol Sci, 2023, 19(3):981-993] PubMed: 36778120
Galectin-9 blockade synergizes with ATM inhibition to induce potent anti-tumor immunity [ Int J Biol Sci, 2023, 19(3):981-993] PubMed: 36778120
Serine/threonine kinase TBK1 promotes cholangiocarcinoma progression via direct regulation of β-catenin [ Oncogene, 2023, 42(18):1492-1507] PubMed: 36928362
Regulation of Synovial γδ T Cell Ligand Expression by Mitochondrial Reactive Oxygen Species and Gasdermin-D [ J Immunol, 2023, 210(1):61-71] PubMed: 36445376
FACT subunit SUPT16H associates with BRD4 and contributes to silencing of interferon signaling [ Nucleic Acids Res, 2022, 50(15):8700-8718] PubMed: 35904816
MD2 deficiency prevents high-fat diet-induced AMPK suppression and lipid accumulation through regulating TBK1 in non-alcoholic fatty liver disease [ Clin Transl Med, 2022, 12(3):e777] PubMed: 35343085
Molecular mechanism of RIPK1 and caspase-8 in homeostatic type I interferon production and regulation [ Cell Rep, 2022, 41-1:111434] PubMed: 36198273

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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.