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