SML3352
GSK973
≥98% (HPLC)
Synonym(s):
(2S,3S)-N5-((1R,5S,6r)-3-oxabicyclo[3.1.0]hexan-6-yl)-2-(fluoromethyl)-N7-methyl-3-phenyl-2,3-dihydrobenzofuran-5,7-dicarboxamide
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About This Item
Empirical Formula (Hill Notation):
C23H23FN2O4
CAS Number:
Molecular Weight:
410.44
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.21
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Related Categories
Biochem/physiol Actions
Orally available, potent and selective pan-second bromodomain (BD2) inhibitor that effectively inhibits LPS-induced MCP-1 release in human whole blood.
GSK973 is an orally available, potent and selective pan-second bromodomain (BD2) inhibitor (BD2/BD1 pIC50 = 7.5/4.4/BRD2, 7.8/4.5/BRD3, 7.8/4.6/BRD4, 7.4/4.5/BRDT) that effectively inhibits LPS-induced MCP-1 release in human whole blood (pIC50 = 7.3; IC50 = 50 nM).
GSK973 is an orally available, potent and selective pan-second bromodomain (BD2) inhibitor (BD2/BD1 pIC50 = 7.5/4.4/BRD2, 7.8/4.5/BRD3, 7.8/4.6/BRD4, 7.4/4.5/BRDT) that effectively inhibits LPS-induced MCP-1 release in human whole blood (pIC50 = 7.3; IC50 = 50 nM).
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Alex Preston et al.
ACS medicinal chemistry letters, 11(8), 1581-1587 (2020-08-25)
Pan-BET inhibitors have shown profound efficacy in a number of in vivo preclinical models and have entered the clinic in oncology trials where adverse events have been reported. These inhibitors interact equipotently with the eight bromodomains of the BET family
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