GSK8612 | Highly selective TBK1 inhibitor

GSK8612 is a highly selective and potent (avg. pIC50 = 6.8 versus recombinant TBK1) inhibitor of Tank-binding Kinase-1 (TBK1) with higher affinity for unactivated TBK1.  It inhibited phosphorylation of IRF3 (pIC50 = 6.0), inhibited the release of IFNa from human PBMC’s (pIC50 = 6.1), and inhibited IFNb secretion from THP-1 cells (pIC50 = 5.8 dsDNA virus, 6.3 cGAMP stilmulated cells).

Reference:

  1. Thomson et al. (2019), Discovery of a GSK8612, a Highly Selective and Potent TBK1 Inhibitor; ACS Med. Chem. Lett., 10 780
Weight 0.01 mg
Dimensions 0.01 × 0.01 × 0.01 cm
Size:

5 mg, 25 mg

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CAS:
2361659-62-1
Catalog Number:
10-4693
Activity:
Highly selective TBK1 inhibitor
Chemical Names:
4-[[[5-Bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
Molecular Weight:
520.33
Molecular Formula:
C17H17F3N7O2S
Solubility:
Soluble in DMSO (20 mg/ml)
Physical Properties:
Beige solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

GSK8612 | Highly selective TBK1 inhibitor

$95.00$370.00

CAS:
2361659-62-1
Catalog Number:
10-4693
Activity:
Highly selective TBK1 inhibitor
Chemical Names:
4-[[[5-Bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
Molecular Weight:
520.33
Molecular Formula:
C17H17F3N7O2S
Solubility:
Soluble in DMSO (20 mg/ml)
Physical Properties:
Beige solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
  • 5 mg
  • 25 mg
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