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  3. GSK8612

GSK8612 

Cat. No.: HY-111941 Purity: 98.37%
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
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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Based on 1 publication(s) in Google Scholar

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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 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 (IFN) in response to dsDNA and cGAMP, the natural ligand for STING[1].

Molecular Weight

520.33

Formula

C₁₇H₁₇BrF₃N₇O₂S

CAS No.

2361659-62-1

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
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GSK8612
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HY-111941
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