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SML2721

GSK8612

≥98% (HPLC)

Synonym(s):

4-(((5-Bromo-2-((3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)amino)methyl)benzenesulfonamide, 4-((5-Bromo-2-(3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-ylamino)pyrimidin-4-ylamino)methyl)benzenesulfonamide, GSK 8612, GSK-8612

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About This Item

Empirical Formula (Hill Notation):
C17H17BrF3N7O2S
CAS Number:
2361659-62-1
Molecular Weight:
520.33
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD32062739
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

FC(F)(F)C[n]1nc(c(c1)Nc2nc(c(cn2)Br)NCc3ccc(cc3)[S](=O)(=O)N)C

InChI key

FFPHMUIGESPOTK-UHFFFAOYSA-N

Biochem/physiol Actions

GSK8612 is a potent and highly selective tank-binding kinase-1 (TBK1) inhibitor (pIC50 = 6.8; pKd = 8.0 vs pKa = 6.2/STK17B, 6.0/IKKε, 6.1/LRRK2, 6.0/FLT4, 5.8/ULK3, 5.7/BMP2K, 5.7/CSNK2A1, 5.6/CSNK2A2, 5.6/FLT4, 5.5/PIK3CD, <5.5/more than 270 kinases). GSK8612 inhibits IFNβ secretion induced by dsDNA containing virus or STING ligand cGAMP (IC50 = 1.25 & 0.5 μM, respectively; THP-1), as well as suppresses TLR3 ligand poly(I:C)-induced IRF3 Ser396 phosphorylation (IC50 = 1 μM; Ramos) and IFNα release (IC50 = 0.79 μM; human PBMCs), a IFN positive feedback response steming from IFNβ.
Potent and highly selective tank-binding kinase-1 (TBK1) inhibitor.

Storage Class

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

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