YK-4-279

For research use only.

Catalog No.S7679

6 publications

YK-4-279 Chemical Structure

CAS No. 1037184-44-3

YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).

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Selleck's YK-4-279 has been cited by 6 publications

1 Customer Review

  • 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.

    Oncotarget, 2017, 8(55):94780-94792. YK-4-279 purchased from Selleck.

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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]

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 29212266     


Cell cytotoxicity of YK-4-279 of NB cells in the CCK-8 assay. Six human NB cell lines SK-N-AS, SH-SY5Y, CHLA-255, NB-19, NGP, and IMR-32 were treated with YK-4-279 at the concentrations of 0, 0.01 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM, and 100 μM for 72 h, and then subjected to a CCK-8 assay. The absorbance of each well was measured at 450 nm and plotted for the cell viability curve. The data are represented as mean ± SD. IC50 values of YK-4-279 in NB cell lines are listed.

29212266
Western blot
PARP / Cleaved PARP / Caspase 3 / Cleaved Caspase 3 ; 

PubMed: 29212266     


YK-4-279-induced cell apoptosis of NB cells by Western blot assay. SK-N-AS 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.

p-HH3(Ser10) / Histone H3 / p-Aurora A (T288) / Aurora A / Aurora B / Cyclin B / p53 / p21 ; 

PubMed: 28602975     


SK-N-AS, GIMEN and NF-730 were treated with DMSO (D) or two doses of YK-4-279 for 24 h and protein lysates harvested. Blots were probed for several cell cycle and cell death markers. All neuroblastoma cell lines showed increase of phospho-histone H3 (Ser10(pHH3), cleaved PARP and active caspase-3. Actin was used as a loading control. 

29212266 28602975
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]

Protocol

Animal Research:[1]
- Collapse
  • Animal Models: Nude mice bearing prostate cancer PC3, TC71 or CHP-100 xenografts
  • Dosages: 1.5 mg/dose
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL (199.34 mM)
Ethanol 51 mg/mL warmed (139.26 mM)
Water 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 Information

Molecular Weight 366.20
Formula

C17H13Cl2NO4

CAS No. 1037184-44-3
Storage powder
in solvent
Synonyms N/A
Smiles COC1=CC=C(C=C1)C(=O)CC2(C3=C(C=CC(=C3NC2=O)Cl)Cl)O

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    I would like to know whether YK-4-279 is the racemate version, or whether it is the + R-enantiomer or the – S-enantiomer of the compound?

  • Answer:

    For our S7679 YK-4-279, it is a recemate.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID