YK-4-279 1037184-44-3

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Molecular Weight:

366.20 YK-4-279 is a Potent Inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).

Biological Activity

YK-4-279 eliminates cyclin D levels by blocking the interaction of
EWS-FLI1 with RHA in EWS-FLI1-containing TC32 cells. YK-4-279 also
specifically inhibits ESFT cell growth and induces Apoptosis.


YK-4-279 also inhibits ERG and ETV1 biological activity in
fusion-positive prostate cancer cells, and further decreases cell
motility and invasion.


In vivo, YK-4-279 (1.5 mg/dose i.p.) inhibits the growth of ESFT xenograft tumors. In mouse model, YK-4-279 selectively prevents prostate cancer growth and metastasis in fusion-positive LNCaP-luc-M6 tumors.






Plasmids and reporter assay


The NR0B131 luciferase reporter and full-length EWS-FLI1 are transiently
transfected into COS-7 cells with Fugene-6 and luciferase assay
performed per manufacturer's protocol (Dual Luciferase Kit). Six hours
following transfection, cells are treated with either 3 or 10 μM
YK-4-279.


Cell lysates luciferase activity levels are standardized to
renilla activity from a non-affected promoter and plotted as relative
luciferase activity (RLA).

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Product Categories : DNA Damage > DNA/RNA Synthesis Inhibitor