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Gimeracil

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Chemical Structure| 103766-25-2 同义名 : 吉美拉西 ;Gimestat;CDHP;chlorodihydroxypyridine. Abbreviation: CDHP.;5-Chlorodihydropyrimidine
CAS号 : 103766-25-2
货号 : A230901
分子式 : C5H4ClNO2
纯度 : 98%
分子量 : 145.544
MDL号 : MFCD08458352
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(721.43 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Dehydrogenase
描述 Gimeracil (5-chloro-2, 4-dihydroxypyridine) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood. 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[3]. Results of gamma-H2AX focus assay indicated that 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[4]. Gimeracil and radiation combination treatment significantly inhibited OSCC (oral squamous cell carcinoma) cell/tumor growth and colony formation. Down-regulated expressions of DNA double-strand break repair proteins were observed in gimeracil and/or radiation treated cells/tumors[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

6.87mL

1.37mL

0.69mL

34.35mL

6.87mL

3.44mL

68.71mL

13.74mL

6.87mL
参考文献

[1]Sakata K, Someya M, 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, Sakata K, et al. Gimeracil sensitizes cells to radiation via inhibition of homologous recombination. Radiother Oncol. 2010 Aug;96(2):259-66.

[3]Sakata K, Someya M, Matsumoto Y, Tauchi H, Kai M, Toyota M, Takagi M, Hareyama M, Fukushima M. Gimeracil, an inhibitor of dihydropyrimidine dehydrogenase, inhibits the early step in homologous recombination. Cancer Sci. 2011 Sep;102(9):1712-6

[4]Takagi M, Sakata K, Someya M, Tauchi H, Iijima K, Matsumoto Y, Torigoe T, Takahashi A, Hareyama M, Fukushima M. Gimeracil sensitizes cells to radiation via inhibition of homologous recombination. Radiother Oncol. 2010 Aug;96(2):259-66

[5]Harada K, Ferdous T, Ueyama Y. Gimeracil Exerts Radiosensitizing Effects on Oral Squamous Cell Carcinoma Cells In Vitro and In Vivo. Anticancer Res. 2016 Nov;36(11):5923-5930