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    Gimeracil
    Gimeracil

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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 #: V0866
    CAS #: 103766-25-2Purity ≥98%

    Description: Gimeracil (chlorodihydroxypyridine; CDHP; Gimestat), a pyridine/pyridone analog and an approved anticancer drug, is a potent inhibitor of the dihydropyrimidine dehydrogenase (DPYD) enzyme with potential anti-neoplastic activity. It is used as an adjunct to or in combination with other anticancer therapeutics to increase the systemic concentrations and therapeutic effectiveness of other antineoplastic drugs. Gimeracil inhibits the early steps in homologous recombination for double strand breaks repair of DNA.  

    References: Oncol Rep. 2010 Nov;24(5):1307-13; Cancer Sci. 2011 Sep;102(9):1712-6

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    Molecular Weight (MW)145.54
    FormulaC5H4ClNO2
    CAS No.103766-25-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 29 mg/mL (199.3 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: 5-chloro-2-hydroxypyridin-4(1H)-one
    InChi Key: ZPLQIPFOCGIIHV-UHFFFAOYSA-N
    InChi Code: InChI=1S/C5H4ClNO2/c6-3-2-7-5(9)1-4(3)8/h1-2H,(H2,7,8,9)
    SMILES Code: O=C1C=C(O)NC=C1Cl
    Synonyms

    Gimestat, chlorodihydroxypyridine; CDHP; Gimeracil 


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    In Vitro

    In vitro activity:  Gimeracil had radiosensitizing effects by partially inhibiting homologous recombination (HR) in the repair of DNA double strand breaks.  Tail moments in neutral comet assay increased in gimeracil-treated cells. Gimeracil restrained the formation of foci of Rad51 and replication protein A (RPA), whereas it increased the number of foci of Nbs1, Mre11, Rad50, and FancD2. Gimeracil did not sensitize DPYD-depleted cells. Gimeracil inhibited DNA DSB repair. It did not sensitize cells deficient in HR but sensitized those deficient in NHEJ. In SCneo assay, Gimeracil reduced the frequency of neo-positive clones. Additionally, it sensitized the cells in S-phase more than in G0/G1.


    Kinase Assay: Gimeracil(Gimestat) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood; inhibits homologous recombination.


    Cell Assay: Gimeracil had radiosensitizing effects by partially inhibiting homologous recombination (HR) in the repair of DNA double strand breaks. Tail moments in neutral comet assay increased in gimeracil-treated cells. Gimeracil restrained the formation of foci of Rad51 and replication protein A (RPA), whereas it increased the number of foci of Nbs1, Mre11, Rad50, and FancD2. Gimeracil did not sensitize DPYD-depleted cells. Gimeracil inhibited DNA DSB repair. It did not sensitize cells deficient in HR but sensitized those deficient in NHEJ. In SCneo assay, Gimeracil reduced the frequency of neo-positive clones. Additionally, it sensitized the cells in S-phase more than in G0/G1.

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    ReferencesOncol Rep. 2010 Nov;24(5):1307-13; Cancer Sci. 2011 Sep;102(9):1712-6 


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

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