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Cycloheximide

现货
Catalog No.
A8244
抗生素,真核生物蛋白质合成抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
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200mg
¥ 500.00
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500mg
¥ 700.00
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1g
¥ 1,100.00
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5g
¥ 3,400.00
现货

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Background

IC50: N/A

Cycloheximide is an inhibitor of protein biosynthesis in eukaryotic organisms widely used in biomedical research to inhibit protein synthesis in eukaryotic cells studied in vitro. Due to significant toxic side effects, including teratogenesis, DNA damage, and other reproductive effects, cycloheximide is generally used only in in vitro research applications, but not suitable for human use as a therapeutic compound.

In vitro: Cycloheximide blocks the movement of peptidyl-tRNA from acceptor site to the donor site on reticulocyte ribosomes. This translocation reaction is dependent on the transfer enzyme, TF-II, and GTP hydrolysis. Cycloheximide has no effect on the ribosome dependent GTPase activity of TF-II or peptidyl transferase reaction by which peptides on tRNA in the donor ribosomal site are transferred to an amino acid on tRNA in the acceptor site [1].

In vivo: Cycloheximide treatment was effective in attenuating rat brain injury within a 6 hr therapeutic window after hypoxia-ischemia in a newborn rat pup model. These data support the possibility that protein synthesis inhibitors, as well as other anti-apoptotic strategies, may have therapeutic utility in hypoxic-ischemic (HI) events of the developing newborn brain even when treatment is delayed for up to 6 hr after the primary asphyxial insult [2].

Clinical trial: Up to now, cycloheximide is still in the preclinical development stage.

References:
[1] McKeehan W, Hardesty B.  The mechanism of cycloheximide inhibition of protein synthesis in rabbit reticulocytes. Biochem Biophys Res Commun. 1969 Aug 15;36(4):625-30.
[2] Park WS, Sung DK, Kang S, Koo SH, Kim YJ, Lee JH, Chang YS, Lee M.  Therapeutic window for cycloheximide treatment after hypoxic-ischemic brain injury in neonatal rats. J Korean Med Sci. 2006 Jun;21(3):490-4.

文献引用

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt281.4
Cas No.66-81-9
FormulaC15H23NO4
SynonymsNaramycin A; Actidione; 3-[2-(3,5-Dimethyl-2-oxocyclohexyl)-2-hydroxyethyl]glutarimide
Solubility≥14.07 mg/mL in DMSO, ≥57.6 mg/mL in EtOH, ≥14.05 mg/mL in H2O with ultrasonic and warming
Chemical Name4-[(2R)-2-[(1S,3S,5S)-3,5-dimethyl-2-oxocyclohexyl]-2-hydroxyethyl]piperidine-2,6-dione
SDFDownload SDF
Canonical SMILESCC1CC(C(=O)C(C1)C(CC2CC(=O)NC(=O)C2)O)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验: [1]

细胞系

SGBS前脂肪细胞

制备方法

该化合物在DMSO中的溶解度大于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

10 μg/ml,9 hours

实验结果

在加入CHX 1、3、6和9小时后,CHX增强CD95诱导的caspase-8裂解为p43/p41中间体和p18活性片段,以及caspase-8的酶原形式的蛋白水解周转。此外,在这些时间点,CHX增加caspase-3切割成活性p20/17片段。在稍后的时间点(24、48和72小时),p55原形式的caspase-8和p35原形式的caspase-3减少。有趣的是,尽管在24小时后没有诱导细胞死亡,但是α-APO-1单独诱导caspase-8和caspase-3切割(3、6、9小时)。通过使用caspase抑制剂Z-VAD.fmk,证实caspase切割参与其中,其减少CD95-和CHX-诱导的细胞凋亡。在SGBS前脂肪细胞中,CHX抑制了约50%的凋亡,表明存在不依赖于caspase的细胞死亡。

动物实验: [2]

动物模型

Sprague Dawley 新生大鼠

给药剂量

腹腔注射,0.6 mg/kg,0、6、12 或24 hr

实验结果

建立大鼠幼仔缺氧缺血模型,缺氧缺血对照组(HI)和缺氧缺血(HI)处理后0、6、12和24小时(HI_0、6、12、24)用CHX处理的缺氧缺血组。在通过TTC对梗死面积的形态分析发现,在HI后0或6小时给予CHX时,梗塞体积分别降低92%和61%,但是与HI对照组相比,如果HI 12小时后施用CHX,梗塞减少趋势不明显,当给药延迟至HI后24小时,没有观察到保护作用。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1] Fischer-Posovszky P, Keuper M, Nagel S, et al. Downregulation of FLIP by cycloheximide sensitizes human fat cells to CD95-induced apoptosis. Experimental cell research, 2011, 317(15): 2200-2209.

[2] Park W S, Sung D K, Kang S, et al. Therapeutic window for cycloheximide treatment after hypoxic-ischemic brain injury in neonatal rats. Journal of Korean medical science, 2006, 21(3): 490-494.

生物活性

描述 Cycloheximide是一种高度有效的抗生素。
靶点 bacteria protein synthesis          
IC50            

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