SML4052

GSK023

Name: GSK023
Brand: SIGMA

≥98% (HPLC)

别名:

(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

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关于此项目

经验公式（希尔记法）:

C₂₉H₃₉N₅O₂

分子量:

489.65

UNSPSC Code:

12352200

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

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).