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.
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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 |
++
R132H-IDH1, IC50: 70 nM R132C-IDH1, IC50: 0.16 μM |
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 (rat), IC50: 3 nM SCD1 (mouse), IC50: 1 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。 |
靶点 |
|
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]. |
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 |
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 |