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    YK-4-279
    YK-4-279

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1436
    CAS #: 1037184-44-3Purity ≥98%

    Description: YK-4-279 (YK-4279; YK4279; YK4-279; YK 4-279) is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA) with potential anticancer activity. It inhibits protein-protein interactions between ES-FLI1 and RHA. YK-4-279 effectively antagonizes EWS-FLI1 induced leukemia in a transgenic mouse model. YK-4-279 demonstrates specificity in targeting the oncogene EWS-FLI1. 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.

    References: Nat Med. 2009 Jul;15(7):750-6; PLoS One. 2014 Dec 5;9(12):e114260. 

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    Molecular Weight (MW)366.20 
    FormulaC17H13Cl2NO4 
    CAS No.1037184-44-3 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 73 mg/mL (199.3 mM)
    Water: <1 mg/mL
    Ethanol: 51 mg/mL (139.3 mM) 
    Other info

    Chemical Name: 4,7-dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-2H-indole-2-one

    InChi Key: HLXSCTYHLQHQDJ-UHFFFAOYSA-N

    InChi Code: InChI=1S/C17H13Cl2NO4/c1-24-10-4-2-9(3-5-10)13(21)8-17(23)14-11(18)6-7-12(19)15(14)20-16(17)22/h2-7,23H,8H2,1H3,(H,20,22)

    SMILES Code: O=C1NC2=C(C(Cl)=CC=C2Cl)C1(O)CC(C3=CC=C(OC)C=C3)=O

    Synonyms

    YK-4-279; YK-4279; YK4279; YK4-279; YK 4-279; YK 4279.


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    In Vitro

    In vitro 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 VivoIn 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. 
    Animal modelNude mice bearing prostate cancer PC3, TC71 or CHP-100 xenografts 
    Formulation & DosageDissolved in DMSO; 1.5 mg/dose; i.p. injection
    References

    Nat Med. 2009 Jul;15(7):750-6; PLoS One. 2014 Dec 5;9(12):e114260.  


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    YK-4-279

    PLoS One. 2014 Dec 5;9(12):e114260.
     

    YK-4-279

    PLoS One. 2014 Dec 5;9(12):e114260.


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