3-MA (3-Methyladenine)

别名: NSC 66389 中文名称:3-甲基腺嘌呤

3-MA (3-Methyladenine)是一种选择性PI3K抑制剂,作用于Vps34PI3Kγ,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

3-MA (3-Methyladenine) Chemical Structure

CAS: 5142-23-4

规格 价格 库存 购买数量
50mg 579.66 现货
500mg 3010.37 现货
2g 6470.1 现货
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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


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

相关信号通路图

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 3-MA (3-Methyladenine)是一种选择性PI3K抑制剂,作用于Vps34PI3Kγ,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!
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

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) Warmed with 50°C water bath; Ultrasonicated; ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 10 mg/mL (67.04 mM)

Water : 4 mg/mL (26.81 mM)

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

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)

mg/kg g μL

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,: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: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: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.

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