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    PRT4165
    PRT4165

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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 #: V0083
    CAS #: 31083-55-3Purity ≥98%

    Description: PRT4165 (NSC600157) is a potent inhibitor of the PRC1 (polycomb repressive complex 1)-mediated H2A ubiquitylation with an IC50 of 3.9 µM in a cell-free assay. It inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro. PRT4165 also inhibits the accumulation of all detectable ubiquitin at sites of DNA double-strand breaks (DSBs), the retention of several DNA damage response proteins in foci that form around DSBs, and the repair of the DSBs.  PRC1-mediated histone ubiquitylation plays an important role in aberrant gene silencing in human cancers and is a potential target for cancer therapy. PRT4165 as a novel chromatin-remodeling compound provides a new tool for the inhibition of ubiquitylation signaling at DNA double-strand breaks.

    References:  2013 Sep 13;288(37):26944-54. 

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    Molecular Weight (MW) 235.24
    Formula C15H9NO2
    CAS No. 31083-55-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 11 mg/mL (46.8 mM)
    Water: 4 mg/mL (17.0 mM)
    Ethanol: < 1 mg/mL 
    Chemical Name 2-(3-Pyridinylmethylene)-1H-Indene-1,3(2H)-dione
    Synonyms PRT4165, PRT-4165, PRT 4165; NSC600157; NSC 600157; NSC-600157
    SMILES Code O=C1/C(C(C2=C1C=CC=C2)=O)=C\C3=CC=CN=C3


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    In Vitro

    In vitro activity: In vitro E3 ubiquitin ligase activity assays revealed that PRT4165 inhibits both RNF2 and RING 1A, which are partially redundant paralogues that together account for the E3 ubiquitin ligase activity found in PRC1 complexes, but not RNF8 nor RNF168. 


    Kinase Assay:


    Cell Assay: Cells are treated with different concentrations of the PRT4165 60 min prior to irradiation (2 Gy). The cells are harvested 2 h after IR. The cells are washed with PBS twice and then fixed with 1% paraformaldehyde at 37°C for 10 min. After cooling on ice for 1 min, the cells are permeabilized with 90% methanol and stored at -20°C overnight. Fixed cells are washed with PBS twice and blocked with FACS incubation buffer (0.5% BSA in PBS) for 10 min. The cells are then stained with anti-phosphohistone H3 (serine 10) antibody at 1:500 dilution in FACS incubation buffer for 1 h at room temperature. 

    In VivoInhibition of PRC1 causes alteration of gene regulation and polyploidy development during decidualization in vivo.
    Animal model CD-1 mice
    Formulation & Dosage Dissolved in sesame oil containing 10% ethanol; 4 mg/kg and 8 mg/kg; intraluminally injection
    References  2013 Sep 13;288(37):26944-54; . 2016; 6: 26061.


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

    PRT4165


    PRT4165 inhibits the PRC1 E3 monoubiquitin ligase activity toward γ-H2AX in vivo.  2013 Sep 13;288(37):26944-54.

     PRT4165


    PRT4165 does not inhibit the E3 ubiquitin ligase activity of RNF8 in vitro.  2013 Sep 13;288(37):26944-54.

     PRT4165


    Effect of PRT5165 on G2/M DNA damage checkpoints and DSB repair.  2013 Sep 13;288(37):26944-54. 

     PRT4165


    PRT 4165 inhibits K63 polyubiquitin chains IRIF in cells.  2013 Sep 13;288(37):26944-54.

     PRT4165


    Effect of PRT5165 on the localization of 53BP1 and BRAC1 into sites of DNA damage.  2013 Sep 13;288(37):26944-54. 

     PRT4165


    Inhibition of PRC1 activity in cells delays recovery from genotoxic stress.  2013 Sep 13;288(37):26944-54.


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