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Enzymes for Research, Diagnostic and Industrial Use

AS-252424

Cat No.
CEI-0088
Description
AS-252424, a ATP-competitive and selective small-molecule PI3K-gamma inhibitor, can potently inhibit PI3K-gamma with IC50 of 33 nM .
CAS No.
900515-16-4
Molecular Weight
305.28
Purity
>99%
Storage
2 years at -20 centigrade
Targets
PI3K-gamma
Molecular Formula
C14H8FNO4S
Chemical Name
(Z)-5-((5-(4-fluoro-2-hydroxyphenyl)furan-2-yl)methylene)thiazolidine-2,4-dione
Solubility
DSMO 61 mg/mL Water
In vitro
AS-252424, a ATP-competitive and selective small-molecule PI3K-gamma inhibitor, can potently inhibit PI3K-gamma with IC50 of 33 nM . By inhibiting PI3K-gamma, AS-252424 can decrease Ca 2+ in HL-1 cell mouse cardiomyocytes. AS252424 also can decrease the proliferation of 5 medulloblastoma cell lines, including DAOY and PFSK cells in a dose-dependent manner, with IC50 values in the range of 1 to 15 umol/L. But AS252424 do not shows strong inhibition to cell lines with low PI3K-gamma expression. In addition, 24-hour-treatment with AS252424 enhanced cisplatin-induced apoptosis in medulloblastoma cells.
In vivo
Oral administration of AS-252424 in a mouse model of acute peritonitis led to a significant reduction of leukocyte recruitment.
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