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
In vivo (Add solvents to the product individually and in order)
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.
* <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.)

Preparing Stock Solutions

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 this compound 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, 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[1].
In vivo

This compound 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.

References

  • https://pubmed.ncbi.nlm.nih.gov/31097999/
  • https://pubmed.ncbi.nlm.nih.gov/33679751/

Selleck's GSK8612 Has Been Cited by 26 Publications

Microbial metabolite drives ageing-related clonal haematopoiesis via ALPK1 [ Nature, 2025, 10.1038/s41586-025-08938-8] PubMed: 40269158
Reconstitution of BNIP3/NIX-mitophagy initiation reveals hierarchical flexibility of the autophagy machinery [ Nat Cell Biol, 2025, 27(8):1272-1287] PubMed: 40715440
TBK1 is a signaling hub in coordinating stress-adaptive mechanisms in head and neck cancer progression [ Autophagy, 2025, 1-23.] PubMed: 40114316
Anti-galectin-9 therapy synergizes with EGFR inhibition to reprogram the tumor microenvironment and overcome immune evasion [ J Immunother Cancer, 2025, 13(7)e010926] PubMed: 40664443
Cholesterol 25-Hydroxylase Enhances Myeloid-Derived Suppressor Cell (MDSC) Immunosuppression via the Stimulator of Interferon Genes (STING)-Tank-Binding Kinase 1 (TBK1)-Receptor-Interacting Protein Kinase 3 (RIPK3) Pathway in Colorectal Cancer [ MedComm (2020), 2025, 6(10):e70411] PubMed: 41020041
Anti-herpetic tau preserves neurons via the cGAS-STING-TBK1 pathway in Alzheimer's disease [ Cell Rep, 2025, 44(1):115109] PubMed: 39753133
TBK1 phagosomal recruitment enhances antifungal immunity via positive feedback regulation with SRC [ Cell Rep, 2025, 44(7):115972] PubMed: 40638388
AKT and EZH2 inhibitors kill TNBCs by hijacking mechanisms of involution [ Nature, 2024, 10.1038/s41586-024-08031-6] PubMed: 39385030
Control of mitophagy initiation and progression by the TBK1 adaptors NAP1 and SINTBAD [ Nat Struct Mol Biol, 2024, 31(11):1717-1731] PubMed: 38918639
TBK1-Zyxin signaling controls tumor-associated macrophage recruitment to mitigate antitumor immunity [ EMBO J, 2024, 10.1038/s44318-024-00244-9] PubMed: 39304793

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.