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PD-1/PD-L1抗体抑制剂（Pembrolizumab，Atezolizumab，Nivolumab）重磅上市！
3-Methyladenine (3-MA)
3-Methyladenine (3-MA)
目录号：S2767
别名： NSC 66389
Molecular Weight(MW): 149.15
3-Methyladenine (3-MA)是一种选择性PI3K抑制剂，作用于Vps34和PI3Kγ，在 HeLa细胞中IC50分别为25 μM和60 μM；永久性抑制I型PI3K，但对III型PI3K的抑制是短暂的，也会阻断自噬体的形成。
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客户购买Selleck的此次产品后发表的文献7篇：
客户使用该产品的4个实验数据：
MDC-labeled vacuoles were induced by AZD2014 and inhibited by autophagy inhibitor (3-MA). SMMC-7721 cells were treated with AZD2014 or rapamycin at concentrations of 100 and 600 nM, respectively, for 48 hours in the presence or absence of 3-MA, and then stained with MDC. Cells were immediately observed under a confocal microscope. Cells in the control group were treated with DMSO. bars, 20 μm.
Am J Cancer Res, ): 125-139.
3-Methyladenine (3-MA) purchased from Selleck.
Cells were treated with DMSO, TDCIPP (100 μM) only, or pretreated with 3-MA before treatment with TDCIPP (100 μM). LC3 conversion and beclin-1 and p62 expression were assessed by western blotting at 24 h
Food Chem Toxicol, 3-196.
3-Methyladenine (3-MA) purchased from Selleck.
PC-9/ER cells were treated with CX-4945 (5 mM) for 48 h in the presence or absence of 3-MA (2 mM) and Atg7 siRNA (100 nM). Cleavage of PARP-1 and caspase-3 was shown by Western blot analysis. CT: without
CX-4945; CX: CX-4945; CX+G: CX-4945 + CX+E: CX-4945 + erlotinib.
PLoS One, ): e114000 .
3-Methyladenine (3-MA) purchased from Selleck.
A: The survival ratio of AML12 cells was measured after treatment with rapamycin or 3-MA; B: Western blot was used to detect the expression of LC3 and P62 in AML12 cells treated with Rapamycin or 3-MA.
World J Gastroenterol, ): ..
3-Methyladenine (3-MA) purchased from Selleck.
产品安全说明书
PI3K抑制剂选择性比较
3-Methyladenine (3-MA)是一种选择性PI3K抑制剂，作用于Vps34和PI3Kγ，在 HeLa细胞中IC50分别为25 μM和60 μM；永久性抑制I型PI3K，但对III型PI3K的抑制是短暂的，也会阻断自噬体的形成。
Vps34 (HeLa cells)
PI3Kγ (HeLa cells)
3-MA对Vps34轻微的偏向性可能是由于Vps34中某个特异性的疏水环形结构可以环绕在3-MA的3-甲基基团外面造成的
。据报道对于正常培养和饥饿处理的癌细胞3-MA都能引起细胞死亡。3-MA还可以不通过抑制自吞噬来抑制细胞迁移和入侵，这表明3-MA 除了抑制自吞噬之外还有其它生物功能。3-MA可以造成半胱天冬酶依赖的细胞死亡，这一功能与它对自吞噬的抑制无关。用5mM 3-MA处理葡萄糖饥饿Hela细胞可降低gfp-lc3阳性细胞比例至23%。3-MA处理细胞12到48小时内 LC3-I 的水平上升而LC3-II 水平下降。LC3-I转为为 LC3-II 的过程被3-MA抑制了。 2.5 mM 或5 mM 3-MA 处理HeLa 细胞一天并不影响细胞存活率, 而 10 mM 3-MA 处理一天会造成细胞存活率下降25.0% 。 2.5, 5 或 10 mM 3-MA 处理细胞两天分别使细胞存活率下降 11.5%, 38.0% 和79.4% 。3-MA 降低细胞存活率的作用具有时间和剂量依赖特性。3-MA 明显缩短nocodazole诱导的前中期阻断时间。3-MA 通过抑制自吞噬来抑制SU11274诱导的细胞死亡。 在野生型MEF细胞中延长 3-MA处理时间 (最多 9 小时) 明显造成 LC3 I 到 II 转换。延长 3-MA处理时间会明显增加GFP-LC3的聚集而wortmannin不具有此功能。3-MA介导的LC3 转换和游离 GFP 释放是ATG7依赖的。 3-MA处理会导致 p62 蛋白水平明显升高。即使在Atg5-/- 的MEF细胞中3-MA 也会使p62 水平升高，就像在DOX介导的ATG5缺失的细胞中一样 。3-MA以不同方式抑制 I 型和 III型 PI3K。与野生型细胞相比，在Tsc2-/-细胞中3-MA诱导的 LC3 I 到 LC3 II 转换过程大幅下降。3-MA会破坏mTOR复合物1的拮抗自吞噬功能。
Cell Lines
Assay Type
Concentration
Incubation Time
Formulation
Activity Description
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Microglia&
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3-Methyladenine (3-MA)可以通过对磷酸肌醇3磷酸激酶(PI3K) 的作用来阻断自吞噬, 而PI3K的活性对于自噬体形成早期膜池的成核和组装是必须的。与SAH 处理组相比3-MA并不会改变出血的程度。与SAH +对照成分组相比经过3-MA预处理后会明显加重神经病学症状。3-MA处理会减少自吞噬发生。 相反地,在SAH + 3-MA组里 断裂的半胱天冬酶表达量明显上调，与此一致的是与SAH + 对照成分组相比，SAH + 3-MA组中右脑皮层里原位末端标记阳性细胞数量明显增多。
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
激酶实验：
Protein degradation assay:
HeLa cells are radiolabeled for 24 hours with 0.05 mCi/mL l-[U- 14C]valine. At the end of the labeling period, cells are rinsed three times with PBS. Cells are incubated for the designated times in either full medium or EBSS with or without the presence of 10 mM 3-Methyladenine.
细胞实验：
Cell lines: HeLa 细胞系
Concentrations: 1-10 mM
Incubation Time: 3 分钟
Method: 用台盼蓝染色法分析细胞存活率（如HeLa细胞）。简言之, 经过3-MA处理后将贴壁的与漂浮的细胞都用PBS( pH 7.4)重悬，密度控制在每毫升1-2&times106。加入等体积的0.4% 台盼蓝并彻底混匀。室温孵育3分钟后用血细胞计数器对细胞计数分析。(Only for Reference)
动物实验：
Animal Models: 体重 300-350 g 的成年雄性Sprague–Dawley 大鼠
Formulation: 生理盐水配制
Dosages: 400 nM
Administration: 脑室给药(Only for Reference)
溶解度 (25°C)
(67.04 mM)
(26.81 mM)
(20.11 mM)
从左到右依次将纯溶剂加入产品，现配现用：
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
3 years -20&C powder
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
连续稀释计算器方程
分子量计算器
通过输入化合物的化学式来计算其分子量：
总分子量：g/mol
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
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*留言内容：
常见问题及建议解决方法
I'm also wondering whether it can be dissolved in water,or maybe something like culture medium,normal saline solution to form 10mM solution
As the reference (http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal. pone.0035665), 3-MA, which was found to inhibit autophagy at concentrations ranging from 1 to 10 mM
was directly dissolved into the culture medium at the indicated concentrations. And we tested the solubility of S2767, and found the solubility of 3-MA in DMEM is 31 mg/mL at about 40&C.
Related Antibodies
PI3K Inhibitors with Unique Features
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