product name Gimeracil
Description: Gimeracil is a potent inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair of DNA. Gimeracil is a pyridine derivative with anticancer/tumor activity. Gimeracil also enhances the antitumor activity of fluoropyrimidines by competitively and reversibly inhibiting the enzyme dihydropyrimidine dehydrogenase causing decreased degradation of the fluoropyrimidines.
References: Oncol Rep. 2010 Nov;24(5):1307-13; Cancer Sci. 2011 Sep;102(9):1712-6
145.54
Formula
C5H4ClNO2
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
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19410488
| 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: |
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| In Vivo | |
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| Formulation & Dosage | |
| References | Oncol Rep. 2010 Nov;24(5):1307-13; Cancer Sci. 2011 Sep;102(9):1712-6 |
