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    ME0328 (ME-0328)
    ME0328 (ME-0328)

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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 #: V0312
    CAS #: 1445251-22-8Purity ≥98%

    Description: ME0328 (ME-0328) is a novel, potent and selective inhibitor of Poly (ADP-ribose) polymerase (PARP) with potential anticancer activity. It inhibits PARP3 with an IC50 of 0.89 μM, and is about 7-fold more selective over PARP1 (IC50 = 6.3 μM).  

    References: ACS Chem Biol. 2013 Aug 16;8(8):1698-703.

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    Molecular Weight (MW)321.37
    FormulaC19H19N3O2
    CAS No.1445251-22-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 64 mg/mL (199.1 mM)
    Water:<1 mg/mL 
    Ethanol: <1 mg/mL
    Other infoChemical Name: 3-(4-oxo-1H-quinazolin-2-yl)-N-[(1S)-1-phenylethyl]propanamide

    InChi Key: QIHBWVVVRYYYRO-ZDUSSCGKSA-N

    InChi Code: InChI=1S/C19H19N3O2/c1-13(14-7-3-2-4-8-14)20-18(23)12-11-17-21-16-10-6-5-9-15(16)19(24)22-17/h2-10,13H,11-12H2,1H3,(H,20,23)(H,21,22,24)/t13-/m0/s1

    SMILES Code: O=C(N[[email protected]](C1=CC=CC=C1)C)CCC(NC2=C3C=CC=C2)=NC3=O

    SynonymsME 0328; ME0328; ME-0328.


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    In Vitro

    In vitro activity: ME0328 is soluble, cell permeable, and metabolically stable in human liver microsomes and rat hepatocytes. ME0328 (10 μM) results in a significant delay of γH2AX-foci resolution by affecting ARTD3 in A549 and MRC5 cells without significant toxicity.


    Kinase Assay: Protein ADP-ribosylation is measured using hexahistidine-tagged ARTD proteins and recombinant histone proteins captured on 96-well Ni2+-chelating plates (5-PRIME). ADP-ribosylation reactions are initiated by addition of NAD+ (2% biotinylated), and modified reaction products are detected by chemiluminescence. Km values are estimated using plots of initial rates vs. NAD+ concentrations and linear curve fitting with GraphPad Prism. All compounds are dissolved in dimethyl sulfoxide (DMSO) to a stock concentration of 50 mM. Experiments to determine IC50 values are conducted with compound concentrations in the range between 10 nM and 450 μM with a DMSO concentration of 1% (v/v). Measurements are carried out at an NAD+ concentration below Km for each transferase. IC50 values are estimated using curve fitting with GraphPad Prism. Reported values represent means ± SE of the fits of the curves based on duplicate or triplicate experiments, each determined based on three replicates. 


    Cell Assay: Compound cytotoxicity in A549 and MRC5 cells is evaluated using WST-1 assays. A549 cells are cultured in Dulbecco’s Modified Eagle’s Medium supplemented with 10% fetal calf serum (FCS), penicillin, and streptomycin. MRC5 cells are cultured in Minimal Essential Medium supplemented with 10% FCS, penicillin, streptomycin, and l-glutamine. Both cell lines are maintained in a humidified incubator at 37°C and 5% CO2.

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    Formulation & DosageNA
    References

    ACS Chem Biol. 2013 Aug 16;8(8):1698-703.


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

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