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3-Methyladenine

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Chemical Structure| 5142-23-4 同义名 : 3-甲基腺嘌呤 ;3-MA;NSC 66389;3-Methyladenine, NSC 66389
CAS号 : 5142-23-4
货号 : A145872
分子式 : C6H7N5
纯度 : 98%
分子量 : 149.153
MDL号 : MFCD00010531
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 7 mg/mL(46.93 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

H2O: 5 mg/mL(33.52 mM)，配合低频超声助溶
动物实验配方：

IP 2% DMSO+water 0.4 mg/mL clear

PO 0.5% CMC-Na 66 mg/mL suspension

生物活性
靶点

  • p110γ

    PI3Kγ, IC50:60 μM

  • Vps34

    Vps34, IC50:25 μM
描述 Vps34 is one kind of PI3K isoform, which plays an essential role in endosomal trafficking of proteins to the vacuole/lysosome, autophagy and phagocytosis. 3-Methyladenine (3-MA) shows inhibition of Vps34 in vitro, with an IC50 of 25 μM as compared with 60 μM for PI3Kγ. 3-Methyladenine is typically employed at a concentration of 10 mM in cellular studies[1]. It is usually served as the inhibitor for both autophagy[1] and type 1 mitophagy through suppression of class III PI3K activity [2]. However, now it was found that 3-Methyladenine play a dual role in modulation of autophagy. Prolonged treatment with 3-Methyladenine (5mM) up to 9 h can induce LC3 I to II conversion in wild type MEFs, L929 and 293T cells cultured in full-medium, whereas it is still effective in suppressing LC3 II conversation in cells induced by starvation. And this observation is consistent with result of punctuate formation of GFP-LC3 study. These results demonstrate that prolonged treatment with 3-Methyladenine under nutrient-rich conditions can enhance autophagic flux. This may due to its different temporal patterns of inhibition on Class I and III PI3K[3].
作用机制 May due to the specific hydrophobic ring to Vps34 encircles the 3-methyl group of 3-MA.[1]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
1321N1 5mM Cytotoxicity Assay 24h protects cell against PCN-induced toxicity 23525265
95D 3mM Growth Inhibition Assay 2h reduces growth inhibitory effect of BDMC 25716561
95D 5mM Apoptosis Assay 2h inhibits BDMC-induced apoptotic cell death 25716561
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

6.70mL

1.34mL

0.67mL

33.52mL

6.70mL

3.35mL

67.05mL

13.41mL

6.70mL
参考文献

[1]Miller S, Oleksy A, et al. Finding a fitting shoe for Cinderella: searching for an autophagy inhibitor. Autophagy. 2010;6(6):805-7.

[2]Petiot A, Ogier-Denis E, et al. Distinct classes of phosphatidylinositol 3'-kinases are involved in signaling pathways that control macroautophagy in HT-29 cells. J Biol Chem. 2000;275(2):992-8.

[3]Wu YT, Tan HL, et al. Dual role of 3-methyladenine in modulation of autophagy via different temporal patterns of inhibition on class I and III phosphoinositide 3-kinase. J Biol Chem. 2010;285(14):10850-61.

[4]Liu H, Lei H, et al. Autophagy inhibitor 3-methyladenine alleviates overload-exercise-induced cardiac injury in rats. Acta Pharmacol Sin. 2017;38(7):990-997.

[5]Slavin SA, Leonard A, et al. Autophagy inhibitor 3-methyladenine protects against endothelial cell barrier dysfunction in acute lung injury. Am J Physiol Lung Cell Mol Physiol. 2018;314(3):L388-L396.