Gimeracil

Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase (DYPD; Ki = 0.36 µM), the rate limiting enzyme in the catabolism of pyrimidines, including 5-fluorouracil (5-FU; Item No. 14416).1 It inhibits the degradation of 5-FU in rat liver extracts (IC50 = 0.1 µM). Gimeracil inhibits homologous recombination and enhances radiation-induced cell death in DLD-1 human colorectal cancer cells.2 Formulations containing gimeracil have been used in conjunction with 5-fluorouracil in the treatment of various cancers.WARNING This product is not for human or veterinary use.

A DYPD inhibitor

145.5

≥98%

Biochemicals/Small Molecule Inhibitors/Nucleic Acid Turnover/Signaling

Formal_Name:5-chloro-4-hydroxy-2(1H)-pyridinone;Synonyms:CDHP 5-Chlorodihydropyrimidine Gimestat

ClC(C(O)=C1)=CN([H])C1=O

C5H4ClNO2

103766-25-2

≥ 4 years

DMF: 20 mg/ml DMSO: 25 mg/ml DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml Ethanol: 0.1 mg/ml

1.Wyatt, M.D. and Wilson, D.M., III. Participation of DNA repair in the response to 5-fluorouracil. Cell Mol.Life Sci. 66(5), 788-799 (2009).
2.Adjei, A.A. A review of the pharmacology and clinical activity of new chemotherapy agents for the treatment of colorectal cancer. British Journal of Clinical Pharmacology 48(3), 265-277 (1999).
3.Sakata, K.I.,Someya, M.,Matsumoto, Y., et al. Gimeracil, an inhibitor of dihydropyrimidine dehydrogenase, inhibits the early step in homologous recombination. Cancer Science 102(9), 1712-1716 (2011).