3-Methyladenine

SKU: orb1307279

特色

描述

3-Methyladenine (3-MA) is an autophagy inhibitor functioning through the inhibition of class III PI3K VPS34 (IC50=25 μM) and class IB PI3Kγ (IC50=60 μM). It is widely used as a pharmacological tool in both in vitro and in vivo studies to investigate autophagic pathways in cancer, neurodegeneration, and other cellular processes.

研究领域

Cell Biology

图片与验证

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关键属性

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CAS 号	5142-23-4
MW	149.2
纯度	>98%
分子式	C₆H₇N₅
SMILES	NC1=C2N=CN=C2N(C)C=N1
靶点	Kinase
溶解性	Soluble in Water (up to 5 mg/ml), or in DMSO (up to 3 mg/ml), or in DMF (up to 10 mg/ml).

生物活性

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靶点 IC50	PI3Kγ:60 μM (HeLa cells)\|MIAPaCa2 cells:> 100 μM\|VPS34:25 μM (HeLa cells)\|Autophagy:1.21 mM
体内	METHODS: To investigate the effects of 3-Methyladenine on atherosclerosis, 3-Methyladenine (30 mg/kg) was injected intraperitoneally into HFD-fed ApoE-/- mice twice weekly for eight weeks. RESULTS: In mice fed a high-fat diet, 3-Methyladenine treatment significantly reduced the size of atherosclerotic plaques and increased the stability of the lesions. 3-Methyladenine has multiple atheroprotective effects on atherosclerosis, including modulation of macrophage autophagy and foam cell formation as well as alteration of the immune microenvironment. METHODS: To investigate the regulatory role of autophagy, a single dose of 3-Methyladenine (15 mg/kg ) was administered intraperitoneally to LPS-induced endotoxic shock in C57/BL6 mice. RESULTS: Animals treated with LPS in combination with 3-Methyladenine showed increased survival and decreased serum inflammatory mediators TNF-α and IL-6 after endotoxemia.
体外	METHODS: Human cervical cancer cells HeLa were treated with 3-Methyladenine (2.5-10 mM) for 48 h. Cell growth inhibition was detected by Trypan blue dye exclusion assay. RESULTS: 3-Methyladenine decreased HeLa cell viability in a time- and dose-dependent manner. METHODS: Adipocytes 3T3-L1 were treated with 3-Methyladenine (5 mM) for 4 h in the absence of serum, and the expression levels of target proteins were detected by Western Blot. RESULTS: 3-Methyladenine significantly decreased the intracellular level of LC3-II, a marker of autophagy, and increased the expression of p62, indicating that 3-Methyladenine was effective in inhibiting autophagy. METHODS: Mouse melanoma cells B16 were treated with 2DG (5 mM), rotenone (1 μM) and 3-Methyladenine (1.2-5 mM) for 24 h. Cytotoxicity was detected by LDH release assay. RESULTS: 3-Methyladenine dose-dependently reduced the up-regulation of LDH release induced by 2DG/rotenone. 3-Methyladenine protected tumor cells from inhibition of glycolysis and mitochondrial respiration.
细胞研究	Cells were seeded in an 8-well coverglass-bottomed chamber for 24 hours (6×10^3 cells per well). Images were acquired automatically at multiple locations on the coverglass using a Nikon TE2000E inverted microscope fitted with a 20× Nikon Plan Apo objective, a linearly-encoded stage, and a Hamamatsu Orca-ER CCD camera. A mercury-arc lamp with two neutral density filters (for a total 128-fold reduction in intensity) was used for fluorescence illumination. The microscope was controlled using NIS-Elements Advanced Research software and housed in a custom-designed 37°C chamber with a secondary internal chamber that delivered humidified 5% CO2. Fluorescence and differential interference contrast images were obtained every 10 min for a period of 48 hours. To analyze live cell imaging movies, the time-lapse records of live cell imaging experiments were exported as an image series and analyzed manually using NIS-Elements Advanced Research software. The criteria for analyses were described previously, and lagging chromosomes in prometaphase were defined as the red fluorescence-positive materials that lingered outside the roughly formed metaphase plate for more than 3 frames (30 min) .
动物研究	All rats were fasted for 12 h with free access to water prior to operation. After anesthesia by intraperitoneal (i.p.) injection of 2% sodium pentobarbital (0.25 mL/100 g), they were laid and fixed on the table, routinely shaven, disinfected, and draped. The rat SAP model was induced by 0.1 mL/min speed uniformly retrograde infusion of a freshly prepared 3.5% sodium taurocholate solution (0.1 mL/100 g) into the biliopancreatic duct after laparotomy. Equivalent volume of normal saline solution was substituted for 3.5% sodium taurocholate solution in the sham-operation (SO) control group. The incision was closed with a continuous 3-0-silk suture, and 2 mL/100 g of saline was injected into the back subcutaneously to compensate for the fluid loss. 180 rats were randomly divided into four groups: (1) Acanthopanax treatment group (Aca group, n = 45) where the rats were injected with 0.2% Acanthopanax injection at a dose of 3.5 mg/100 g 3 h after successful modeling via the vena caudalis once, knowing that this dosage was effective as proven in our previous experiment; (2) 3-Methyladenine treatment group (3-methyladenine group, n = 45) where the rats were injected with 100 nmol/μL 3-methyladenine solution at a dose of 1.5 mg/100 g 3 h after successful modeling via the intraperitoneal route once, knowing that this dosage was effective as proven in the literature ; (3) SAP model group (SAP group, n = 45) where these rats received an equivalent volume of the normal saline instead of Acanthopanax injection 3 h after successful modeling via the vena caudalis once; (4) SO group (control, n = 45) where these rats received an equivalent volume of the normal saline instead of Acanthopanax injection 3 h after successful sham-operation via the vena caudalis once. The 45 animals in each of the four groups were equally randomized into 3, 12, and 24 h subgroups for postoperative observations .

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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3-MA

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质量保证

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化合物标识

PubChem CID

135398661 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

反应性：	Human
动态范围：	0.16-10 ng/mL
灵敏度：	0.06 ng/mL

应用：	ELISA, IHC, WB
反应性：	Human
种属/宿主：	Rabbit
克隆性：	Polyclonal
偶联：	Unconjugated

应用：	ELISA, WB
反应性：	Human
种属/宿主：	Rabbit
克隆性：	Polyclonal
偶联：	Unconjugated

应用：	WB
反应性：	Human, Mouse, Rat
种属/宿主：	Rabbit
克隆性：	Polyclonal
偶联：	Unconjugated

3-Methyladenine

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

Human N-Methylpurine DNA Glycosylase (MPG) ELISA Kit [orb777103]

MPG Antibody [orb520320]

MPG Rabbit Polyclonal Antibody [orb2955296]

MPG Antibody [orb520321]

MPG Rabbit Polyclonal Antibody [orb214270]

质量保证

化合物标识

关键属性

实验方案信息

可选规格