A TBK1 inhibitor
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GSK8612

Item No. 28813

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]amino]-4-pyrimidinyl]amino]methyl]-benzenesulfonamide
CAS Number
2361659-62-1
Molecular Formula
C17H17BrF3N7O2S
Formula Weight
520.3
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mLDMSO: 5 mg/mLPBS (pH 7.2): 0.3 mg/mL
λmax
228 nm
SMILES
NS(C1=CC=C(CNC2=C(Br)C=NC(NC3=CN(CC(F)(F)F)N=C3C)=N2)C=C1)(=O)=O
InChi Code
InChI=1S/C17H17BrF3N7O2S/c1-10-14(8-28(27-10)9-17(19,20)21)25-16-24-7-13(18)15(26-16)23-6-11-2-4-12(5-3-11)31(22,29)30/h2-5,7-8H,6,9H2,1H3,(H2,22,29,30)(H2,23,24,25,26)
InChi Key
FFPHMUIGESPOTK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $74

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    10 mg

    $132

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    25 mg

    $293

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    50 mg

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    Product Description

    GSK8612 is an inhibitor of TANK-binding kinase 1 (TBK1; IC50 = 158 nM).1 It is selective for TBK1 over a panel of 285 kinases. GSK8612 inhibits IFN-α release in isolated human peripheral blood mononuclear cells (PBMCs) stimulated with polyinosinic-polycytidylic acid (poly(I:C); IC50 = 794 nM). It also inhibits IFN-β secretion in THP-1 cells stimulated with dsDNA-containing baculovirus or cGAMP (IC50s = 1,258 and 501 nM, respectively). GSK8612 (5 mg/kg) reduces tumor volume and increases the number of tumor-infiltrating CD8+ T cells in immunocompetent, but not immunodeficient, mice in a model of carbon tetrachloride-induced hepatocellular carcinoma (HCC).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Thomson, D.W., Poeckel, D., Zinn, N., et al. Discovery of GSK8612, a highly selective and potent TBK1 inhibitor. Med. Chem. Lett. 10(5), 780-785 (2019).

    2. Jiang, Y., Chen, S., Li, Q., et al. TANK-binding kinase 1 (TBK1) serves as a potential target for hepatocellular carcinoma by enhancing tumor immune infiltration. Front. Immunol. 12, 612139 (2021).