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吉美嘧啶 /Gimeracil {[allProObj[0].p_purity_real_show]}

货号:A230901 同义名: 吉美拉西 / Gimestat;CDHP

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

Gimeracil 化学结构 CAS号:103766-25-2
Gimeracil 化学结构
CAS号:103766-25-2
Gimeracil 3D分子结构
CAS号:103766-25-2
Gimeracil 化学结构 CAS号:103766-25-2
Gimeracil 3D分子结构 CAS号:103766-25-2
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Gimeracil 纯度/质量文件 产品仅供科研

货号:A230901 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Dehydrogenase 其他靶点 纯度
Trilostane 99+%
AGI-6780 +++

IDH2 R140Q mutant, IC50: 23 nM

99%+
Gimeracil 98%
AGI-5198 ++

R132C-IDH1, IC50: 0.16 μM

R132H-IDH1, IC50: 70 nM

99%+
SW033291 ++++

15-PGDH, IC50: 1.5 nM

15-PGDH, Ki: 0.1 nM

99%+
Mycophenolic acid 99+%
Fomepizole 98%
Leflunomide 98%
3-Nitropropanoic acid 99%+
Isovaleramide 98%
Mycophenolate Mofetil +++

Inosine monophosphate dehydrogenase I, IC50: 39 nM

Inosine monophosphate dehydrogenase II, IC50: 27 nM

98%
MK-8245 ++++

SCD1 (mouse), IC50: 1 nM

SCD1 (rat), IC50: 3 nM

99%+
Vidofludimus ++

Human DHODH, IC50: 134 nM

99%+
Emodin 98%
Ivosidenib 98%
NCT-501 ++

ALDH1A1, IC50: 40 nM

98%
Gossypol 99%+
Devimistat 98%
Disulfiram 98%+
Enasidenib ++++

IDH2, IC50: 12 nM

98%
PluriSIn 1 99%+
ML390 +

DHODH, IC50: 0.56 μM

99%+
Teriflunomide 99%+
Daidzin +++

ALDH-Ⅰ, Ki: 20 nM

98+%
18β-Glycyrrhetinic acid 99%
RRx-001 95%
NCT-503 +

PHGDH, IC50: 2.5 μM

99%+
Vorasidenib 99%+
Ammonium Glycyrrhizinate(x:1) 98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Gimeracil 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].

Gimeracil 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

Gimeracil 实验方案

计算器
存储液制备 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

Gimeracil 技术信息

CAS号103766-25-2
分子式C5H4ClNO2
分子量 145.544
别名 吉美拉西 ;Gimestat;CDHP;chlorodihydroxypyridine. Abbreviation: CDHP.;5-Chlorodihydropyrimidine
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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