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3-Methyladenine

Cat. No. M2296
3-Methyladenine Structure
Synonym:

3-MA

Size Price Availability Quantity
50mg USD 63 In stock
100mg USD 90 In stock
500mg USD 320 In stock
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Quality Control
Biological Activity

3-Methyladenine is a selective autophagy and phosphoinositide 3-kinase (PI3K) inhibitor for Vps34 and PI3Kγ with IC50 of 25 and 60 nM, respectively. 3-Methyladenine significantly shortens the duration of nocodazole-induced-prometaphase arrest. 3-Methyladenine inhibits class I and class III PI3K in different temporal patterns. 3-Methyladenine blocks autophagy through its effect on class III phosphatidylinositol 3-kinase (PI3K), the activity of which is required for the nucleation and assembly of the initial phagophore membrane. 3-Methyladenine treatment does not alter the degree of hemorrhage compared with the SAH group.

Protocol
Cell Experiment
Cell lines U251 cells
Preparation method Western blotting was performed to determine the expression levels of ubiquitinated proteins, PDI and Grp78. The expression levels of ubiquitinated PDI and Grp78 were increased following the inhibition of autophagy by treatment with 3-MA
Concentrations 10 mM
Incubation time 12 h
Animal Experiment
Animal models Male Wistar rats
Formulation saline
Dosages 3.5 mg/kg
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 149.15
Formula C6H7N5
CAS Number 5142-23-4
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Int J Clin Exp Med (2017) . Figure 6. 3-methyladenine (3-MA) (Abmole Bioscience Inc. Houston, TX, USA)
Method Evaluation of the inhibitory activity
Cell Lines Human NSCLC cell line NCI-H1975
Concentrations 100 mM
Incubation Time
Results In addition, the suppression of mTOR phosphorylation decreased the percentage of early apoptotic cells (Figure 6A and 6B) and caspase 3 cleavage (Figure 6C).
Rating
Source Int J Clin Exp Med (2017) . Figure 5. 3-methyladenine (3-MA) (Abmole Bioscience Inc. Houston, TX, USA)
Method Evaluation of the inhibitory activity
Cell Lines Human NSCLC cell line NCI-H1975
Concentrations 100 mM
Incubation Time
Results As a control, 3-MA was used to prevent mTOR phosphorylation. The suppression of mTOR phosphorylation decreased the number of intracellular autophagosomes increased by treatment with wogonin plus icotinib combination (Figure 5B).
Rating
Source Mol Immunol (2017) . Figure 2. 3-methyladenine (Abmole Bioscience, USA)
Method IL-37 induces autophagy in SMMC-7721 and Huh-7 cells.
Cell Lines SMMC-7721 and Huh-7 cells
Concentrations 5 mmol/l
Incubation Time
Results The LC3-II/LC3-I ratio was significantly decreased in IL-37/3-MA-co-treated SMMC-7721 and Huh-7 cells and increased in IL-37/CQ-co-treated SMMC-7721 and Huh-7 cell (Fig. 2E and F). Together, these data further indicate that IL-37 induces autophagy in SMMC-7721 and Huh-7 cells.
Rating
Source Tianjin Med J (2016). 3-MA, Figure 4. (AbMole, USA)
Method MTT实验
Cell Lines A549 细胞
Concentrations 5 μmol/L
Incubation Time 24 h
Results 与阴性对照组比较,在作用48、72、96 h 后 Neratinib 及3-MA 能有效抑制A549 细胞的增殖(F 分别为15.213 4.965、5.366,均P<0.05),见图4。
Rating
Source Tianjin Med J (2016). 3-MA, Figure 3. (AbMole, USA)
Method Transwell invasion
Cell Lines A549 细胞
Concentrations 5 μmol/L
Incubation Time 24 h
Results Neratinib 处理组、3-MA 处理组穿膜细胞数分别为40±8、59±10,均显著低于阴性对照组的113±13,差异均有统学意义(F=18.246,P<0.05),见图3。提示HER2 低表达及细胞自噬活性水平降低能抑制肺癌细胞系A549 细胞侵袭。
Rating
Source Tianjin Med J (2016). 3-MA, Figure 2. (AbMole, USA)
Method Wound healing 实验
Cell Lines A549 细胞
Concentrations 5 μmol/L
Incubation Time 24 h
Results Neratinib 及3-MA 对A549 细胞迁徙能力的影响Neratinib 处理组、3-MA 处理组24 h 迁徙率分别为11.1%±1.4% 10.5%±1.2%,均低于阴性对照组的42.9%±2.4%,差异均有统计学意义(F=27.430,P<0.05),见图2。提HER2 低表达及细胞自噬活性水平能降低抑制肺癌细胞系A549 细胞迁徙。
Rating
Source Tianjin Med J (2016). 3-MA, Figure 1. (AbMole, USA)
Method Western blot
Cell Lines A549 细胞
Concentrations 5 μmol/L
Incubation Time 24 h
Results Neratinib 及3-MA 对A549 细胞自噬相关蛋白 Beclin-1 及LC3B(Ⅱ/Ⅰ)表达的影响与阴性对照 组相比,3-MA 处理组的Beclin-1 蛋白及LC3BⅡ/ Ⅰ表达水平明显降低;Neratinib 处理组的HER2、Beclin-1 蛋白及LC3BⅡ/Ⅰ表达水平明显降低(P<0.05),见图1。提示在人源肺癌A549 细胞中,改变 HER2 的表达能调控细胞自噬的活性。
Rating
Product Citations
References

Inhibition of autophagy using 3-methyladenine increases cisplatin-induced apoptosis by increasing endoplasmic reticulum stress in U251 human glioma cells.
Zhang R, et al. Mol Med Rep. 2015 Aug;12(2):1727-32. PMID: 25846607.

3-methyladenine, an autophagic inhibitor, attenuates therapeutic effects of sirolimus on scopolamine-induced cognitive dysfunction in a rat model.
Zhu B, et al. Int J Clin Exp Med. 2014 Oct 15;7(10):3327-32. PMID: 25419365.

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Keywords: 3-Methyladenine, 3-MA supplier, PI3K, inhibitors

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