3-MA (3-Methyladenine)

别名: NSC 66389 中文名称：3-甲基腺嘌呤

目录号：S2767 Purity: 99.97%

3-MA (3-Methyladenine)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。在溶液中不稳定，请现配现用！

3-MA (3-Methyladenine) Chemical Structure

CAS: 5142-23-4

规格	价格	库存
50mg	RMB 579.66	现货
500mg	RMB 3010.37	现货
2g	RMB 6470.1	现货
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400-668-6834 info@selleck.cn

客户使用Selleck的3-MA (3-Methyladenine)发表文献830篇

产品质控

批次：纯度： 99.97%

99.97

常与3-MA (3-Methyladenine)一起在实验中被使用的化合物

Chloroquine

3-Methyladenine和Chloroquine可阻断MCF-7和HFF细胞中tetrandrine诱导的自噬。

Wang H, et al. Cell Biosci. 2015 Jan 14;5:4.

Rapamycin (Sirolimus)

3-Methyladenine显著抑制LPS处理小鼠的结肠组织自噬，而Rapamycin则诱导自噬。

Zhou M, et al. EBioMedicine. 2018 Sep;35:345-360.

Necrostatin-1

3-Methyladenine和Necrostatin-1抑制LPS/zVAD和PolyI: C/zVAD诱导的骨髓巨噬细胞(BMDM)细胞死亡。

Chen YS, et al. Mol Cells. 2022 Apr 30;45(4):257-272.

Z-VAD-FMK

3-Methyladenine和Z-VAD-FMK联合应用证实了细胞程序性死亡在pristimerin介导的抗癌作用中的重要作用。

Al-Tamimi M, et al. Biomed Pharmacother. 2022 Dec;156:113950.

Fer-1 (Ferrostatin-1)

3-Methyladenine和Ferrostatin-1可消除丙烯酰胺(ACR)诱导的软骨细胞细胞死亡。

Wang H, et al. Exp Ther Med. 2023 Apr 12;25(6):246.

3-MA (3-Methyladenine)相关产品

相关靶点	p110α p110β p110δ p110γ C2β Vps34	点击展开
相关化合物库	激酶抑制剂库 PI3K/Akt 抑制剂库凋亡分子化合物库细胞周期化合物库 NF-κB信号通路库	点击展开

PI3K抑制剂选择性比较

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
SMMC-7721	Apoptosis Assay	5mM	24h	attenuates TNF-α protection against serum starvation-mediated apoptosis	24066693
HO8910	Apoptosis Assay	10mM	12h	enhances B19-induced apoptosi	23983610
MCF7	Function Assay	5mM	24h	increases CuO induced cell death	23962629
HONE-1	Function Assay	5mM	1h	represses 6r-mediated ROS production	23892358
HeLa	Function Assay	10mM	2h	suppresses LC3 II expressison	23864738
HepG2	Function Assay	10mM	24h	inhibits siTIGAR- and HBSS-induced autophagy	23817040
SH-SY5Y	Function Assay	1mM	24h	inhibits the autophagy induced by TOCP	23743148
SH-SY5Y	Apoptosis Assay	5mM	1h	abolishes celastrol neuroprotective effect	23619395
PC12	Function Assay	10mM	24h	inhibits chymotrypsin-like proteasomal activity.	23603979
OV2008	Apoptosis Assay	5mM	24h	converts FTY720 with CDDP into an additive effect towards killing ovarian cancer cells	23592281
A2780	Apoptosis Assay	5mM	24h	converts FTY720 with CDDP into an additive effect towards killing ovarian cancer cells	23592281
1321N1	Cytotoxicity Assay	5mM	24h	protects cell against PCN-induced toxicity	23525265
Saos-2	Apoptosis Assay	1mM	96h	increases cell death induced by PCX	23563171
SH-SY5Y	Cytotoxicity Assay	5mM	24h	increases PCN toxicity	23525265
HT-29	Function Assay	1mM	48/96h	inhibits AMPK induces autophagic cell death	23508272
OR6	Function Assay	10mM	72h	suppresses HCV replication and formation of autophagosomes	23395875
Hela	Function Assay	5mM	24h	inhibits starvation-induced autophagy	23395679
MCF-7	Function Assay	5mM	24h	inhibits starvation-induced autophagy	23395679
HUVECs	Function Assay	3mM	24h	blocks the protective effect of resveratrol by inhibiting autophagy	23358928
T24	Function Assay	10mM	1h	reduces the cleavage of LC3 after baicalin treatment	23354080
U251MG	Function Assay	3mM	1h	suppresses LC3-II protein expression	23338618
GTL-16	Apoptosis Assay	5mM	24h	reduces cell viability as compared to cells treated with MET inhibitors	23313490
T-47D	Function Assay	10mM	2h	inhibits autophagy process and increases rapamycin induced apoptosis	23300026
PaCa44	Apoptosis Assay	2.5mM	1h	reduces genipin-mediated apoptosis	23124112
MDA-MB231	Function Assay	5mM	1h	increases resveratrol-mediated caspase activation and cell death	23088850
SK-HEP-1	Apoptosis Assay	10mM	1h	protects against autophagy and induces apoptosis in bufalin-treated cells	22858649
HeLa	Apoptosis Assay	10mM	2h	decreases cell viability co-treatment with PEI	23000135
HepG2	Apoptosis Assay	3mM	5h	reduces cell apoptosis induced by QDs	22836595
MCF-7	Function Assay	2mM	24h	inhibits autophagy induced by TM	24970676
MCF-7	Function Assay	2mM	48h	promotes TM-induced cell death	24970676
MDA-MB-231	Function Assay	2mM	24h	inhibits autophagy induced by TM	24970676
MDA-MB-231	Function Assay	2mM	48h	promotes TM-induced cell death	24970676
PANC-1	Apoptosis Assay	1mM	48h	enhances bortezomib-induced cell viability loss	24842158
MDA-MB 231	Apoptosis Assay	5mM	0.5h	modulates Tocomin® induced apoptosis	24830781
Microglia	Apoptosis Assay	5mM	24h	decreases hypoxia-induced cell death	24818601
HepG2	Function Assay	5mM	4h	increases cellular levels of HL	24713587
A2780cp	Apoptosis Assay	2.5mM	1h	enhances cisplatin-induced cell death	24817946
U2OS	Growth Inhibition Assay	10mM	24h	intensifies the growth inhibition induced by Dox	24639013
HCT116	Apoptosis Assay	5mM	24h	enhances apigenin-induced cell death	24626522
PC-3	Apoptosis Assay	2mM	2h	increases ORI-induced cell death	22745580
MCF-7	Apoptosis Assay	0.1mM	6h	enhances sirtinol-induced apoptosis	22751989
U251	Apoptosis Assay	5mM	24h	increases S1-induced cell death	22579788
HeLa	Apoptosis Assay	5mM	24h	induces caspase-dependent cell death	22545128
pDCs	Function Assay	10mM	0.5h	reduces the induction of IFN-α by ssRNA40	22396599
A549	Function Assay	0.1mM	24h	suppresses SU11274-induced cell death	22466960
BGC-823	Function Assay	5mM	2h	inhibits the rate of autophagic cells	22322152
U937	Function Assay	2mM	12h	decreases the autophagy ratio	22155150
Marc-145	Function Assay	5mM	12/24/36h	reduces the PRRSV titers and the protein expression	22119900
HBx	Apoptosis Assay	10mM	48h	increases cell death	22020078
MCF-7	Function Assay	10mM	48h	blocks autophagy induced by bortezomib	21931937
RMPI8226	Function Assay	5mM	1h	suppresses the level of autophagy under nutrient depletion	21915620
PC12/TetOn	Function Assay	0.1/1mM	18h	leads to α-syn(WT) accumulation, toxicity, and oligomer formation	21906659
HeLa	Cytotoxicity Assay	2mM	24h	inhibites the cytotoxicity of silibinin to HeLa cells.	21875385
Jurkat	Function Assay	10mM	1h	decreases the expression of LC3-II and the formation of autophagosomes	21864037
K562	Function Assay	10mM	1h	decreases the expression of LC3-II and the formation of autophagosomes	21864037
Hep3B	Apoptosis Assay	5mM	24h	attenuates TNF-α protection against serum starvation-mediated apoptosis	24066693
H460	Function Assay	10mM	4h	increases cisplatin-induced cell death	24173208
A549	Function Assay	10mM	4h	inhibits autophagy induced by irradiation	24142735
H1299	Function Assay	10mM	4h	increases cisplatin-induced cell death	24173208
WiDr	Function Assay	10mM	1h	inhibits PCBL-induced LC3 II expression	24190489
LoVo	Apoptosis Assay	5mM	48h	enhances DCA-induced apoptosis.	24201812
HepG2 E47	Function Assay	2.5mM	48h	increases the toxicity of AA, BSO, and CCl4	24273738
RKO	Function Assay	2mM	1h	enhances cell death by geldanamycin	24291777
Hep3B	Apoptosis Assay	2mM	12h	inhibits AZD8055-induced cell death	24297300
ACHN-5968	Apoptosis Assay	5mM	3h	enhances paclitaxel-mediated apoptosis	24305604
Huh7	Apoptosis Assay	2mM	12h	inhibits AZD8055-induced cell death	24297300
UOK257	Apoptosis Assay	5mM	3h	enhances paclitaxel-mediated apoptosis	24305604
ECSCs	Apoptosis Assay	10mM	4h	decreases rapamycin-treated apoptosis	24319109
MCF-7	Function Assay	10mM	24h	inhibits the autophagy induced by chemotherapy drugs	24315578
SGC-7901	Apoptosis Assay	2mM	1h	increases CA-4 induced apoptosis	24321340
SMMC-7721	Apoptosis Assay	2mM	1h	increases CA-4 induced apoptosis	24321340
T24	Apoptosis Assay	5mM	1.5h	potentiates celecoxib-induced apoptosis	24349176
NTUB1	Apoptosis Assay	5mM	1.5h	potentiates celecoxib-induced apoptosis	24349176
MG-63	Apoptosis Assay	10mM	12h	enhances DP-induced apoptosis	24358301
MG-63	Apoptosis Assay	0.5/1mM	32h	enhances salinomycin-induced cell apoptosis	24358342
MG-63	Function Assay	0.5/1mM	48h	induces salinomycin-induced cell viability loss	24358342
U2OS	Function Assay	0.5/1mM	48h	induces salinomycin-induced cell viability loss	24358342
HGC-27	Function Assay	10mM	1h	inhibits the cell viability loss by RAD001 or MK-2206	24416349
HCT116	Apoptosis Assay	5mM	24h	enhances the apoptosis induced by apigenin	24626522
A549	Apoptosis Assay	10mM	48h	accelerates the reduction of cell viability induced by PTX	24626722
Saos-2	Apoptosis Assay	10mM	24h	intensifies the growth inhibition of the U2OS cells induced by Dox	24639013
U2OS	Apoptosis Assay	10mM	24h	intensifies the growth inhibition of the U2OS cells induced by Dox	24639013
HepG2	Function Assay	5mM	4h	increases HL release	24713587
A549	Apoptosis Assay	5mM	48h	decreases the percentage of cell death and expression levels of caspase-3, Beclin-1 and LC3-II	24706303
A2780cp	Apoptosis Assay	2.5mM	1h	enhances cisplatin-induced cell death	24817946
Microglia	Apoptosis Assay	5mM	24h	decreases hypoxia-induced cell death	24818601
HT-29	Apoptosis Assay	1mM	48h	enhances bortezomib-induced cell viability loss	24842158
MDR	Apoptosis Assay	10mM	6h	strengthens the power of anticancer drugs	25019701
H157	Function Assay	5mM	2h	suppresses SPC induced accumulation of LC3-II	25285628
A549	Function Assay	5mM	2h	suppresses SPC induced accumulation of LC3-II	25285628
A2780cp	Growth Inhibition Assay	1mM	1h	increases cisplatin-induced cell death	25322694
NBL-W-S	Apoptosis Assay	1mM	6h	increases cell apoptosis induced by GANT-61	25323222
NBL-W-S	Growth Inhibition Assay	1mM	6h	enhances GANT-61 toxicity	25323222
A549	Apoptosis Assay	5mM	2h	inhibits BDMC-induced apoptotic cell death	25716561
95D	Apoptosis Assay	5mM	2h	inhibits BDMC-induced apoptotic cell death	25716561
A549	Growth Inhibition Assay	3mM	2h	reduces growth inhibitory effect of BDMC	25716561
95D	Growth Inhibition Assay	3mM	2h	reduces growth inhibitory effect of BDMC	25716561
Nara-H	Growth Inhibition Assay	5mM	48h	enhances temsirolimusmediated suppression of Nara-H cell proliferation	21805033
HUVECs	Function Assay	10mM	0.5h	decreases the AGE-BSAinduced autophagy leve	21468592
HepG2	Apoptosis Assay	2mM	1h	enhances radiation-induced cell death	21453691
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
点击查看更多细胞系数据

生物活性

产品描述

靶点

Autophagy ^[1]	Vps34 ^[1] (HeLa cells)	PI3Kγ ^[1] (HeLa cells)
	25 μM	60 μM

体外研究(In Vitro)
体外研究活性	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^[1] 。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^[2]。3-MA 通过抑制自吞噬来抑制SU11274诱导的细胞死亡^[3]。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^[4]。
细胞实验	细胞系	HeLa 细胞系
	浓度	1-10 mM
	孵育时间	3 分钟
	方法	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1-2×10⁶。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。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	α-SMA / TGF-β / LC-3BI / LC-3B II / Beclin-1 / NF-κB p65 caspase-3 / caspase-9 / PARP VEGF APP / BACE1 / ADAM17 / Presenilin 1 / Presenilin 2 / Nicastrin / APH-1 / Pen-2 / LC3-1 / LC3-2		29296191
	Immunofluorescence	LC3 / Hif-α / COX2		29039446
	Growth inhibition assay	Cell viability		26934124

体内研究(In Vivo)
体内研究活性	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^[5]。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^[5]。
动物实验	Animal Models	体重 300-350 g 的成年雄性Sprague–Dawley 大鼠
	Dosages	400 nM
	Administration	脑室给药

参考文献
[1] Miller S, et al. Autophagy. 2010, 6(6), 805-807. [2] Hou H, et al. PLoS One. 2012, 7(4), e35665. [3] Liu Y, et al. J Pharmacol Sci. 2012, 118(4), 423-432. [4] Wu YT, et al. J Biol Chem. 2010, 285(14), 10850-10861. [5] Jing CH, et al. Neuroscience. 2012. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	149.15	分子式	C₆H₇N₅
CAS号	5142-23-4	SDF	Download 3-MA (3-Methyladenine) SDF
Smiles	CN1C=NC(=N)C2=C1N=CN2
储存条件(自收到货起)	3年 -20°C 粉状	此产品性质不稳定，需现配现用!建议您购买分装规格，或者在收到货后进行分装。

体外溶解度
批次：

DMSO : 10 mg/mL ( (67.04 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 10 mg/mL

Water : 4 mg/mL

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
I'm also wondering whether it can be dissolved in water,or maybe something like culture medium,normal saline solution to form 10mM solution

回答：
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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):