- SML2721
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SML2721
GSK8612
≥98% (HPLC)
All Photos(1)
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
Empirical Formula (Hill Notation):
C17H17BrF3N7O2S
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This Item | SML2770 | SML0428 | SML1960 |
|---|---|---|---|
| assay ≥98% (HPLC) | assay ≥98% (HPLC) | assay ≥98% (HPLC) | assay ≥98% (HPLC) |
| form powder | form powder | form powder | form powder |
| color white to beige | color white to beige | color white to beige | color white to beige |
| solubility DMSO: 2 mg/mL, clear | solubility DMSO: 2 mg/mL, clear | solubility DMSO: 5 mg/mL (clear solution) | solubility DMSO: 20 mg/mL, clear |
| storage temp. 2-8°C | storage temp. −20°C | storage temp. 2-8°C | storage temp. 2-8°C |
| Quality Level 100 | Quality Level 100 | Quality Level 100 | Quality Level 100 |
生物化学的／生理学的作用
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.
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
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