8-Aminoadenosine(Synonyms: 8-氨基腺苷; 8-NH2-Ado)

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8-Aminoadenosine (Synonyms: 8-氨基腺苷; 8-NH2-Ado)

8-Aminoadenosine (8-NH2-Ado) 是一种 RNA 导向的核苷类似物,可降低细胞 ATP 水平并抑制 mRNA 合成。8-Aminoadenosine 阻断 Akt/mTOR 信号,并诱导 p53 非依赖性的自噬和细胞凋亡。8-Aminoadenosine 具有抗肿瘤活性。

8-Aminoadenosine(Synonyms: 8-氨基腺苷; 8-NH2-Ado)

8-Aminoadenosine Chemical Structure

CAS No. : 3868-33-5

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生物活性

8-Aminoadenosine (8-NH2-Ado), a RNA-directed nucleoside analogue, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine blocks Akt/mTOR signaling and induces autophagy and apoptosis in a p53-independent manner. 8-Aminoadenosine has antitumor activity[1][2][3].

IC50 & Target[1][2]

Akt

 

mTOR

 

体外研究
(In Vitro)

8-Aminoadenosine (8-NH2-Ado; 0.1-10 μM; for 48 h) has IC50s of 1.5 μM and 8.88 μM in MM.1S and U266 cells, respectively[1].
8-Aminoadenosine (10 μM; for 24 h) induces significant apoptotic death of MCF-7 cells in p53-independent pathway. 8-Aminoadenosine causes PARP cleavage in MCF-7 cells[2].
8-Aminoadenosine (3 μM; 0.5-4 h) induces autophagy in the MM.1S cell line[1].
8-Aminoadenosine (3 μM; 2-16 h) causes a greater drop in ATP levels in the MM.1S cells[1].
8-Aminoadenosine (3 μM; 5 h) causes a 50% reduction in glucose consumption in MM.1S cells[1].
8-Aminoadenosine (3 μM; 5 h) indicates a time-dependent decrease in GLUT1 expression at 5 h, whereas at 24 h there was a down-regulation of both transporters (GLUT1 and GLUT4) in MM.1S cells[1].
8-Aminoadenosine inhibits cell proliferation, activated cell death, and does not activate transcription of the p53 target gene p21 or increase protein levels of either p53 or p21[1].
The toxic effects of 8-Aminoadenosine require adenosine kinase activity to convert 8-Aminoadenosine to 8-NH2-ATP in adenosine kinase-deficient cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MM.1S and U266 cells
Concentration: 0.1, 0.3, 1, 3, 10 μM
Incubation Time: For 48 hours
Result: Had IC50s of 1.5 μM and 8.88 μM in MM.1S and U266 cells, respectively.

Apoptosis Analysis[2]

Cell Line: MCF-7 cells
Concentration: 10 μM
Incubation Time: For 24 hours
Result: Induced significant apoptotic death.
Apoptosis was not inhibited by knockdown of functional p53.

Apoptosis Analysis[1]

Cell Line: MM.1S cell line
Concentration: 3 μM
Incubation Time: 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4 hours
Result: Induced the formation of LC3-II protein.
Caused the appearance of a population with a high AVO content with 1 μM for 24 hours.

分子量

282.26

Formula

C10H14N6O4

CAS 号

3868-33-5

中文名称

8-氨基腺苷;8-氨基腺苷酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (295.22 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5428 mL 17.7142 mL 35.4283 mL
5 mM 0.7086 mL 3.5428 mL 7.0857 mL
10 mM 0.3543 mL 1.7714 mL 3.5428 mL

参考文献
  • [1]. Mala Shanmugam, et al. Targeting glucose consumption and autophagy in myeloma with the novel nucleoside analogue 8-aminoadenosine. J Biol Chem. 2009 Sep 25;284(39):26816-30.

    [2]. Alla Polotskaia, et al. 8-Amino-adenosine activates p53-independent cell death of metastatic breast cancers. Mol Cancer Ther. 2012 Nov;11(11):2495-504.

    [3]. Jennifer Ann Frey, et al. 8-Amino-adenosine inhibits multiple mechanisms of transcription. Mol Cancer Ther. 2010 Jan;9(1):236-45.

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