1. NF-κB
  2. IKK
  3. GSK8612

GSK8612 

Cat. No.: HY-111941 Purity: 98.79%
Handling Instructions

GSK8612 is a highly selective and potent Tank-binding Kinase-1 (TBK1) inhibitor, with a pIC50 of 6.8 for recombinant TBK1.

For research use only. We do not sell to patients.

GSK8612 Chemical Structure

GSK8612 Chemical Structure

CAS No. : 2361659-62-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 206 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
25 mg USD 590 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GSK8612 purchased from MCE. Usage Cited in: Protein Cell. 2021 Apr;12(4):261-278.

    HEK293T cells are transiently co-transfected for 48 h with Flag-tagged HDAC3 and empty vectors or HA-tagged TBK1 expression plasmids, and treated with GSK8612 for 1 h before co-immunoprecipitation. When TBK1 is treated with its inhibitor GSK8612, the phosphorylation of HDAC3 is significantly decreased.

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    Description

    GSK8612 is a highly selective and potent Tank-binding Kinase-1 (TBK1) inhibitor, with a pIC50 of 6.8 for recombinant TBK1[1].

    IC50 & Target[1]

    TBK1

    6.8 (pIC50)

    In Vitro

    GSK8612 inhibits toll-like receptor (TLR)3-induced IRF3 phosphorylation in Ramos cells and type I IFN secretion in primary human mononuclear cells. In THP1 cells, GSK8612 is able to inhibit secretion of IFNβ in response to dsDNA and cGAMP, the natural ligand for STING[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    520.33

    Formula

    C₁₇H₁₇BrF₃N₇O₂S

    CAS No.
    SMILES

    NS(C1=CC=C(CNC2=C(Br)C=NC(NC3=CN(CC(F)(F)F)N=C3C)=N2)C=C1)(=O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 125 mg/mL (240.23 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9219 mL 9.6093 mL 19.2186 mL
    5 mM 0.3844 mL 1.9219 mL 3.8437 mL
    10 mM 0.1922 mL 0.9609 mL 1.9219 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.00 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (4.00 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.00 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 98.79%

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    Keywords:

    GSK8612GSK 8612GSK-8612IKKIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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    Product Name:
    GSK8612
    Cat. No.:
    HY-111941
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