SML4052

GSK023

≥98% (HPLC)

• Synonym(e): (S)-5-(1-((1-(1-Isopropylpiperidine-4-carbonyl)piperidin-3-yl)-methyl)-1H-benzo[d]imidazole-2-yl)-1,3-dimethylpyridin-2(1H)-one, GSK 023, GSK-023
• Empirische Formel (Hill-System): C₂₉H₃₉N₅O₂
• Molekulargewicht: 489.65
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C

Beschreibung

Biochem/physiol Actions

GSK023 is a potent and selective probe for the N-terminal bromodomain (BD) BD1 of bromodomain and extra-terminal (BET) proteins (pIC50 & BD1/BD2 fold selectivity = 8.0/400/BRD2, 7.7/400/BRD3, 7.8/1000/BRD4, 7.3/630/BRDT by TR-FRET; pKd & BD1/BD2 fold selectivity = 8.5/1000/BRD2, 8.4/400/BRD3, 8.1/316/BRD4, 8.1/400/BRDT by BROMOscan; pKd = 5.0/EP300, >2000/20 non-BET BDs) with antiproliferative potency against human primary T cells, coronary artery smooth muscle cells, endothelial cells, and fibroblasts (0.16-10 µM) by impacting a variety of immune-modulatory biomarkers (MCP-1 pIC50 = 6.9 using human whole blood).

Sicherheitshinweise

• Piktogramme: GHS07
• Signalwort: Warning
• Gefahrencodes: H302,H315
• Sicherheitshinweise: P264 - P280 - P301 + P312 - P302 + P352 - P332 + P313 - P362 + P364
• Hazard Classifications: Acute Tox. 4 Oral - Skin Irrit. 2
• Lagerklasse: 11 - Combustible Solids
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable