YK-4-279

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Technical Data

Molecular Weight 366.20 Storage powder
Formula

C17H13Cl2NO4

in solvent
CAS No. 1037184-44-3 Synonyms N/A
Solubility (25°C) * In vitro DMSO 73 mg/mL (199.34 mM)
Ethanol 51 mg/mL warmed (139.26 mM)
Water Insoluble
In vivo
* <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.
Chemical Name 4,7-dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-2H-indol-2-one

Biological Activity

Description YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).
Targets
RNA helicase A [1]
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. [1] YK-4-279 also inhibits ERG and ETV1 biological activity in fusion-positive prostate cancer cells, and further decreases cell motility and invasion. [2]
In vivo In vivo, YK-4-279 (1.5 mg/dose i.p.) inhibits the growth of ESFT xenograft tumors. [1] In mouse model, YK-4-279 selectively prevents prostate cancer growth and metastasis in fusion-positive LNCaP-luc-M6 tumors. [3]
Features  

Protocol (Only for Reference)

Kinase Assay: [1]

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 Study: [1]

Animal Models Nude mice bearing prostate cancer PC3, TC71 or CHP-100 xenografts
Formulation DMSO
Dosages 1.5 mg/dose
Administration i.p.
 

References

Customer Product Validation

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.

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

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