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Actinomycin D

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Catalog No.
A4448
RNA聚合酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,500.00
现货
5mg
¥ 500.00
现货
10mg
¥ 900.00
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50mg
¥ 3,950.00
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Background

IC50: Actinomycin D showed a concentration-dependent decrease of DNA repair activity with the IC50 of 0.42 μM [1].
Actinomycin D (dactinomycin), a member of actinomycines, which are a class of polypeptide antibiotics isolated from soil bacteria of the genus Streptomyces. Have been used for many years as an older chemotherapy, actinomycin D binds to double- and single-stranded DNA to inhibit DNA and RNA synthesis by binding DNA at the transcription initiation complex and preventing elongation of RNA chain by RNA polymerase.
In vitro: A previous study was designed to determine the effects of actinomycin D on leptin release by isolated rat adipocytes during primary culture for 24 hr. Results showed that both actinomycin D and dexamethasone reduced the loss of leptin mRNA seen over the 24-hr incubation. Maximal effects on leptin release and leptin mRNA accumulation required only 0.1 μM of actinomycin D, a concentration that had no significant effect on the 18S RNA content of adipocytes at the end of a 24-hr incubation. In contrast to the reduced loss of leptin mRNA seen at 24 hr, the loss of glyceraldehyde-3-phosphate dehydrogenase messenger ribonucleic acid (GAPDH mRNA) was enhanced in the presence of 0.1 μM of actinomycin D. These results demonstrated a unique regulation of leptin release and leptin mRNA levels by actinomycin D [2].
In vivo: A rat in vivo study showed that the effect of actinomycin D on the time course of the population spike potentiation was more pronounced than the effect on the time course of the EPSP component, suggesting different mechanisms for the two forms of potentiation. Moreover, both intrahippocampal and intracerebroventricular injection of actinomycin D prevented a late stage of LTP in the dentate gyrus in vivo measured as the population spike amplitude [3].
Clinical trial: Actinomycin is intravenously administered and most commonly used in the treatment of a variety of cancers, including gestational trophoblastic neoplasia, wilms' tumor, rhabdomyosarcoma, ewing's sarcoma and malignant hydatidiform mole. Combined with other drugs in chemotherapy regimens, such as the VAC regimen, it will be used for treating rhabdomyosarcoma and Ewing's Sarcoma. In addition, it is also used as a radiosensitizer in adjunct to radiotherapies, as it increases the tumor cells radiosensitivity.
Reference:
[1] Barret JM, Salles B, Provot C, Hill BT. Evaluation of DNA repair inhibition by antitumor or antibiotic drugs using a chemiluminescence microplate assay. Carcinogenesis. 1997 ;18(12):2441-5.
[2] Fain JN, Bahouth SW. Stimulation of leptin release by actinomycin D in rat adipocytes. Biochem Pharmacol. 1998;55(8):1309-14.
[3] Frey U, Frey S, Schollmeier F, Krug M. Influence of actinomycin D, a RNA synthesis inhibitor, on long-term potentiation in rat hippocampal neurons in vivo and in vitro. J Physiol. 1996;490(Pt 3):703-11.

文献引用

Chemical Properties

StorageDesiccate at 4°C
M.Wt1255.43
Cas No.50-76-0
FormulaC62H86N12O16
SynonymsActD
Solubility≥62.75 mg/mL in DMSO, <6.33 mg/mL in EtOH, <6.28 mg/mL in H2O
Chemical Name2-amino-4,6-dimethyl-3-oxo-1-N,9-N-bis[7,11,14-trimethyl-2,5,9,12,15-pentaoxo-3,10-di(propan-2-yl)-8-oxa-1,4,11,14-tetrazabicyclo[14.3.0]nonadecan-6-yl]phenoxazine-1,9-dicarboxamide
SDFDownload SDF
Canonical SMILESCC1C(C(=O)NC(C(=O)N2CCCC2C(=O)N(CC(=O)N(C(C(=O)O1)C(C)C)C)C)C(C)C)NC(=O)C3=C4C(=C(C=C3)C)OC5=C(C(=O)C(=C(C5=N4)C(=O)NC6C(OC(=O)C(N(C(=O)CN(C(=O)C7CCCN7C(=O)C(NC6=O)C(C)C)C)C)C(C)C)C)N)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

大鼠脂肪细胞

制备方法

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 °C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 °C可放置数月。

反应条件

0、0.1、1或10 μM;24小时

实验结果

在24小时的孵育过程中,Actinomycin D减少瘦素mRNA积累。在浓度为0.1 μM时,Actinomycin D显示出最大抑制作用。

动物实验 [2]:

动物模型

Wistar大鼠

给药剂量

6 μg/μL;海马内或脑室内注射

实验结果

海马内或脑室内注射Actinomycin D减少体内齿状回的LTP晚期阶段。

其它注意事项

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]. Fain JN, Bahouth SW. Stimulation of leptin release by actinomycin D in rat adipocytes. Biochem Pharmacol. 1998;55(8):1309-14.

[2]. Frey U, Frey S, Schollmeier F, Krug M. Influence of actinomycin D, a RNA synthesis inhibitor, on long-term potentiation in rat hippocampal neurons in vivo and in vitro. J Physiol. 1996 Feb 1;490 ( Pt 3):703-11.

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化学结构

Actinomycin D

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