|Solubility (25°C) *||In vitro||DMSO||73 mg/mL (199.34 mM)|
|Ethanol||51 mg/mL warmed (139.26 mM)|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Description||YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).|
|In vitro||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||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).|
|Animal Models||Nude mice bearing prostate cancer PC3, TC71 or CHP-100 xenografts|
Data from [Data independently produced by , , Oncotarget, 2017, 8(55):94780-94792]
YK-4-279-induced cell apoptosis of NB cells by Western blot assay. SH-SY5Y cells were treated with YK-4-279 (0, 0.1 μM, 0.3 μM, 1 μM, 3 μM) for 24 h. Whole cell lysates were subjected to SDS-PAGE and immunoblotted with antibodies against PARP and Caspase 3 to detect apoptosis. β-actin was detected as loading control. YK-4-279-induced apoptosis of NB cell line SH-SY5Y by FACS. Cells were treated with YK-4-279 (0, 1 μM, 3 μM) for 24 h, and then stained by PI and analyzed by FACS.
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