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Gimeracil
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Gimeracil图片
CAS NO:103766-25-2
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
25mg电议

产品介绍
Gimeracil 是口服氟嘧啶衍生物 S-1 的一种成分,可抑制 DNA DSB 修复,是 DPYD(二氢嘧啶脱氢酶,DPD)的有效抑制剂。
Cas No.103766-25-2
别名吉美嘧啶; Gimestat
化学名5-chloro-4-hydroxy-1H-pyridin-2-one
Canonical SMILESC1=C(C(=CNC1=O)Cl)O
分子式C5H4ClNO2
分子量145.54
溶解度≥ 6.6 mg/mL in DMSO, ≥ 6.56 mg/mL in EtOH with ultrasonic and warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Gimeracil(Gimestat) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood; inhibits homologous recombination.IC50 Value: Target: DPYDin vitro: 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 [1]. 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 [2].in vivo:

References:
[1]. Sakata K, et al. Gimeracil, an inhibitor of dihydropyrimidine dehydrogenase, inhibits the early step in homologous recombination. Cancer Sci. 2011 Sep;102(9):1712-6.
[2]. Takagi M, et al. Gimeracil sensitizes cells to radiation via inhibition of homologous recombination. Radiother Oncol. 2010 Aug;96(2):259-66.