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3-MA (3-Methyladenine)

別名: NSC 66389 中文名稱：3-甲基腺嘌呤

3-MA (3-Methyladenine)是一種選擇性PI3K抑制劑，作用于Vps34和PI3Kγ，在 HeLa細胞中IC50分別為25 μM和60 μM；永久性抑制I型PI3K，但對III型PI3K的抑制是短暫的，也會阻斷自噬體的形成。在溶液中不穩(wěn)定，請現配現用！

3-MA (3-Methyladenine) Chemical Structure

3-MA (3-Methyladenine) Chemical Structure

CAS: 5142-23-4

規(guī)格 價格 庫存 購買數量
50mg 579.66 現貨
500mg 3010.37 現貨
2g 6470.1 現貨
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常與3-MA (3-Methyladenine)一起在實驗中被使用的化合物

Chloroquine

3-Methyladenine和Chloroquine可阻斷MCF-7和HFF細胞中tetrandrine誘導的自噬。

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

Rapamycin

3-Methyladenine顯著抑制LPS處理小鼠的結腸組織自噬，而Rapamycin則誘導自噬。

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誘導的骨髓巨噬細胞(BMDM)細胞死亡。

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

Z-VAD-FMK

3-Methyladenine和Z-VAD-FMK聯合應用證實了細胞程序性死亡在pristimerin介導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)誘導的軟骨細胞細胞死亡。

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

3-MA (3-Methyladenine)相關產品

相關信號通路圖

PI3K Signaling Pathways

PI3K信號通路圖

細胞實驗數據示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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生物活性

產品描述 3-MA (3-Methyladenine)是一種選擇性PI3K抑制劑，作用于Vps34和PI3Kγ，在 HeLa細胞中IC50分別為25 μM和60 μM；永久性抑制I型PI3K，但對III型PI3K的抑制是短暫的，也會阻斷自噬體的形成。在溶液中不穩(wěn)定，請現配現用！
靶點
Autophagy [1] Vps34 [1]
(HeLa cells)		 PI3Kγ [1]
(HeLa cells)
25 μM 60 μM
體外研究(In Vitro)
體外研究活性

3-MA對Vps34輕微的偏向性可能是由于Vps34中某個特異性的疏水環(huán)形結構可以環(huán)繞在3-MA的3-甲基基團外面造成的[1] 。據報道對于正常培養(yǎng)和饑餓處理的癌細胞3-MA都能引起細胞死亡。3-MA還可以不通過抑制自吞噬來抑制細胞遷移和入侵，這表明3-MA 除了抑制自吞噬之外還有其它生物功能。3-MA可以造成半胱天冬酶依賴的細胞死亡，這一功能與它對自吞噬的抑制無關。用5mM 3-MA處理葡萄糖饑餓Hela細胞可降低gfp-lc3陽性細胞比例至23%。3-MA處理細胞12到48小時內 LC3-I 的水平上升而LC3-II 水平下降。LC3-I轉為為 LC3-II 的過程被3-MA抑制了。 2.5 mM 或5 mM 3-MA 處理HeLa 細胞一天并不影響細胞存活率, 而 10 mM 3-MA 處理一天會造成細胞存活率下降25.0% 。 2.5, 5 或 10 mM 3-MA 處理細胞兩天分別使細胞存活率下降 11.5%, 38.0% 和79.4% 。3-MA 降低細胞存活率的作用具有時間和劑量依賴特性。3-MA 明顯縮短nocodazole誘導的前中期阻斷時間[2]。3-MA 通過抑制自吞噬來抑制SU11274誘導的細胞死亡[3]。 在野生型MEF細胞中延長 3-MA處理時間 (最多 9 小時) 明顯造成 LC3 I 到 II 轉換。延長 3-MA處理時間會明顯增加GFP-LC3的聚集而wortmannin不具有此功能。3-MA介導的LC3 轉換和游離 GFP 釋放是ATG7依賴的。 3-MA處理會導致 p62 蛋白水平明顯升高。即使在Atg5−/− 的MEF細胞中3-MA 也會使p62 水平升高，就像在DOX介導的ATG5缺失的細胞中一樣 。3-MA以不同方式抑制 I 型和 III型 PI3K。與野生型細胞相比，在Tsc2−/−細胞中3-MA誘導的 LC3 I 到 LC3 II 轉換過程大幅下降。3-MA會破壞mTOR復合物1的拮抗自吞噬功能[4]。
細胞實驗 細胞系 HeLa 細胞系
濃度 1-10 mM
孵育時間 3 分鐘
方法

用臺盼藍染色法分析細胞存活率（如HeLa細胞）。簡言之, 經過3-MA處理后將貼壁的與漂浮的細胞都用PBS( pH 7.4)重懸，密度控制在每毫升1-2×106。加入等體積的0.4% 臺盼藍并徹底混勻。室溫孵育3分鐘后用血細胞計數器對細胞計數分析。
實驗圖片 檢測方法 檢測指標 實驗圖片 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
體內研究(In Vivo)
體內研究活性

3-Methyladenine (3-MA)可以通過對磷酸肌醇3磷酸激酶(PI3K) 的作用來阻斷自吞噬, 而PI3K的活性對于自噬體形成早期膜池的成核和組裝是必須的。與SAH 處理組相比3-MA并不會改變出血的程度。與SAH +對照成分組相比經過3-MA預處理后會明顯加重神經病學癥狀。3-MA處理會減少自吞噬發(fā)生[5]。 相反地,在SAH + 3-MA組里 斷裂的半胱天冬酶表達量明顯上調，與此一致的是與SAH + 對照成分組相比，SAH + 3-MA組中右腦皮層里原位末端標記陽性細胞數量明顯增多[5]。
動物實驗 Animal Models 體重 300-350 g 的成年雄性Sprague–Dawley 大鼠
Dosages 400 nM
Administration 腦室給藥

化學信息&溶解度

分子量 149.15 分子式

C6H7N5
CAS號 5142-23-4 SDF Download 3-MA (3-Methyladenine) SDF
Smiles CN1C=NC(=N)C2=C1N=CN2
儲存條件(自收到貨起) 3年 -20°C 粉狀 此產品性質不穩(wěn)定，需現配現用!建議您購買分裝規(guī)格，或者在收到貨后進行分裝。

體外溶解度
批次：

DMSO : 10 mg/mL ( (67.04 mM) Warmed with 50°C water bath; Ultrasonicated; ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 10 mg/mL (67.04 mM)

Water : 4 mg/mL (26.81 mM)

摩爾濃度計算器

體內溶解度
批次：

現配現用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內配方計算器

實驗計算

摩爾濃度計算器

質量 濃度 體積 分子量

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯系Selleck）；

體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 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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