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M9281 Sigma

3-Methyladenine

autophagy inhibitor

Synonym: 3-MA, 6-Amino-3-methylpurine

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Description

Preparation Note

This product is soluble in DMF (10 mg/ml, may require gentle heating), yielding a clear, colorless solution. It is also soluble in water, 95% ethanol, or 1 N NaOH at 30 mg/ml with heating, but upon cooling, the product precipitates from solution. Solutions of 3-MA are best prepared fresh.

Application

3-Methyladenine (3-MA) is used to inhibit and study the mechanism of autophagy (lysosomal self-degradation) and apoptosis under various conditions. 3-MA inhibits autophagy by blocking autophagosome formation via the inhibition of type III Phosphatidylinositol 3-kinases (PI-3K). For use as an autophagy inhibitor, 3-MA is typically used at a concentration of 5 mM.

Price and Availability

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Safety & Documentation

Protocols & Articles

Articles

Autophagy in Cancer Promotes Therapeutic Resistance

Autophagy is a highly regulated process by which long-lived proteins, organelles, and protein aggregates are captured within autophagosomes, which are then fused with lysosomes for degradation.1 Auto...
Keywords: Apoptosis, Autophagy, Cancer, Degradations, Metabolites, transformation

Peer-Reviewed Papers

References

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α-Synuclein impairs macroautophagy: implications for Parkinson's disease. Winslow AR, Chen CW, Corrochano S, et al. J. Cell Biol. 190(6), 1023-37, (2010)

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ROS-mediated autophagy induced by dysregulation of lipid metabolism plays a protective role in colorectal cancer cells treated with gambogic acid. Zhang H, Lei Y, Yuan P, et al. PLoS ONE 9(5), e96418, (2014)

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Mitigation of autophagy ameliorates hepatocellular damage following ischemia-reperfusion injury in murine steatotic liver. Gupta NA, Kolachala VL, Jiang R, et al. Am. J. Physiol. Gastrointest. Liver Physiol. 307(11), G1088-99, (2014)

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Efavirenz induces neuronal autophagy and mitochondrial alterations. Purnell PR and Fox HS J. Pharmacol. Exp. Ther. 351(2), 250-8, (2014)

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Glucosamine protects nucleus pulposus cells and induces autophagy via the mTOR-dependent pathway. Jiang L, Jin Y, Wang H, et al. J. Orthop. Res. 32(11), 1532-42, (2014)

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Bioenergetic adaptation in response to autophagy regulators during rotenone exposure. Giordano S, Dodson M, Ravi S, et al. J. Neurochem. 131(5), 625-33, (2014)

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G2019S LRRK2 mutant fibroblasts from Parkinson's disease patients show increased sensitivity to neurotoxin 1-methyl-4-phenylpyridinium dependent of autophagy. Yakhine-Diop SM, Bravo-San Pedro JM, Gómez-Sánchez R, et al. Toxicology 324, 1-9, (2014)

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Glucose-starved cells do not engage in prosurvival autophagy. Ramírez-Peinado S, León-Annicchiarico CL, Galindo-Moreno J, et al. J. Biol. Chem. 288(42), 30387-98, (2013)

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Interplay between autophagy and apoptosis in pancreatic tumors in response to gemcitabine. Papademetrio DL, Cavaliere V, Simunovich T, et al. Target. Oncol. 9(2), 123-34, (2014)

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Upexpression of Beclin-1-dependent autophagy protects against beta-amyloid-induced cell injury in PC12 cells. Xue Z, Zhang S, Huang L, et al. J. Mol. Neurosci. 51(1), 180-6, (2013)

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Clearance of the mutant androgen receptor in motoneuronal models of spinal and bulbar muscular atrophy. Rusmini P, Crippa V, Giorgetti E, et al. Neurobiol. Aging 34(11), 2585-603, (2013)

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Autophagy is required and protects against apoptosis during myoblast differentiation. McMillan EM and Quadrilatero J Biochem. J. 462(2), 267-77, (2014)

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Arylpiperazine-mediated activation of Akt protects SH-SY5Y neuroblastoma cells from 6-hydroxydopamine-induced apoptotic and autophagic death. Tovilovic G, Zogovic N, Soskic V, et al. Neuropharmacology 72, 224-35, (2013)

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Mitochondrial translocation of p53 modulates neuronal fate by preventing differentiation-induced mitochondrial stress. Xavier JM, Morgado AL, Solá S, et al. Antioxid. Redox Signal. 21(7), 1009-24, (2014)

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Autophagy promotes radiation-induced senescence but inhibits bystander effects in human breast cancer cells. Huang YH, Yang PM, Chuah QY, et al. Autophagy 10(7), 1212-28, (2014)

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Autophagy inhibition switches low-dose camptothecin-induced premature senescence to apoptosis in human colorectal cancer cells. Zhang JW, Zhang SS, Song JR, et al. Biochem. Pharmacol. 90(3), 265-75, (2014)

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Abberant α-synuclein confers toxicity to neurons in part through inhibition of chaperone-mediated autophagy. Maria Xilouri et al PLoS ONE 4, e5515, (2009)

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Podocyte autophagic activity plays a protective role in renal injury and delays the progression of podocytopathies. Zeng C, Fan Y, Wu J, et al. J. Pathol. 234(2), 203-13, (2014)

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Autophagy-inducing peptides from mammalian VSV and fish VHSV rhabdoviral G glycoproteins (G) as models for the development of new therapeutic molecules. García-Valtanen P, Ortega-Villaizán Mdel M, Martínez-López A, et al. Autophagy 10(9), 1666-80, (2014)

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Autophagy regulates the therapeutic potential of mesenchymal stem cells in experimental autoimmune encephalomyelitis. Dang S, Xu H, Xu C, et al. Autophagy 10(7), 1301-15, (2014)

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Activation of the MAPK11/12/13/14 (p38 MAPK) pathway regulates the transcription of autophagy genes in response to oxidative stress induced by a novel copper complex in HeLa cells. Zhong W, Zhu H, Sheng F, et al. Autophagy 10(7), 1285-300, (2014)

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EGFR inhibitor BIBU induces apoptosis and defective autophagy in glioma cells. Ghildiyal R, Dixit D, and Sen E Mol. Carcinog. 52(12), 970-82, (2013)

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Axonal protection by Nmnat3 overexpression with involvement of autophagy in optic nerve degeneration. Kitaoka Y, Munemasa Y, Kojima K, et al. Cell Death Dis. 4, e860, (2013)

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Suppressing autophagy protects photoreceptor cells from light-induced injury. Zhang TZ, Fan B, Chen X, et al. Biochem. Biophys. Res. Commun. 450(2), 966-72, (2014)

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Autophagy in pulmonary macrophages mediates lung inflammatory injury via NLRP3 inflammasome activation during mechanical ventilation. Zhang Y, Liu G, Dull RO, et al. Am. J. Physiol. Lung Cell. Mol. Physiol. 307(2), L173-85, (2014)

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Autophagy blockade sensitizes the anticancer activity of CA-4 via JNK-Bcl-2 pathway. Li Y, Luo P, Wang J, et al. Toxicol. Appl. Pharmacol. 274(2), 319-27, (2014)

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Bortezomib induces protective autophagy through AMP-activated protein kinase activation in cultured pancreatic and colorectal cancer cells. Min H, Xu M, Chen ZR, et al. Cancer Chemother. Pharmacol. 74(1), 167-76, (2014)

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Comparative study of autophagy inhibition by 3MA and CQ on Cytarabine‑induced death of leukaemia cells. Palmeira dos Santos C, Pereira GJ, Barbosa CM, et al. J. Cancer Res. Clin. Oncol. 140(6), 909-20, (2014)

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The c10orf10 gene product is a new link between oxidative stress and autophagy. Stepp MW, Folz RJ, Yu J, et al. Biochim. Biophys. Acta 1843(6), 1076-88, (2014)

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Suppression of autophagic activation in the mouse uterus by estrogen and progesterone. Choi S, Shin H, Song H, et al. J. Endocrinol. 221(1), 39-50, (2014)

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Autophagy inhibition induces podocyte apoptosis by activating the pro-apoptotic pathway of endoplasmic reticulum stress. Fang L, Li X, Luo Y, et al. Exp. Cell Res. 322(2), 290-301, (2014)

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Single-virus tracking approach to reveal the interaction of Dengue virus with autophagy during the early stage of infection. Chu LW, Huang YL, Lee JH, et al. J. Biomed. Opt. 19(1), 011018, (2014)

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Appropriate modulation of autophagy sensitizes malignant peripheral nerve sheath tumor cells to treatment with imatinib mesylate. Okano M, Sakata N, Ueda S, et al. J. Pediatr. Hematol. Oncol. 36(3), 200-11, (2014)

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Telomelysin shows potent antitumor activity through apoptotic and non-apoptotic cell death in soft tissue sarcoma cells. Li GD, Kawashima H, Ogose A, et al. Cancer Sci. 104(9), 1178-88, (2013)

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MG-2477, a new tubulin inhibitor, induces autophagy through inhibition of the Akt/mTOR pathway and delayed apoptosis in A549 cells. Viola G, Bortolozzi R, Hamel E, Moro S, et al. Biochem. Pharmacol. 83(1), 16-26, (2011)

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Mammalian target of rapamycin regulates isoliquiritigenin-induced autophagic and apoptotic cell death in adenoid cystic carcinoma cells. Chen G, Hu X, Zhang W, Xu N, et al. Apoptosis 17(1), 90-101, (2011)

Inhibition of autophagy by 3-methyladenine protects 1321N1 astrocytoma cells against pyocyanin- and 1-hydroxyphenazine-induced toxicity. McFarland AJ, Anoopkumar-Dukie S, et al. Arch. Toxicol. 86(2), 275-84, (2011)

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Targeting autophagy enhances BO-1051-induced apoptosis in human malignant glioma cells. Chu PM, Chen LH, Chen MT, Ma HI, et al. Cancer Chemother. Pharmacol. 69(3), 621-33, (2011)

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Beil. 26,IV,3564

FT-NMR 1 (3), 217:A / RegBook 1 (2), 2471:F / Structure Index 1, 390:D:8

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