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3-Methyladenine

AG-CR1-3597-M025 25 mg INQ
AG-CR1-3597-M100 100 mg INQ
AG-CR1-3597-M250 250 mg INQ
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Additional Information

Product Data
Synonyms 3-MA; 3MeA; 6-Amino-3-methylpurine; NSC 66389
Properties
Formula C6H7N5
MW 149.2
CAS 5142-23-4
RTECS AU6520000
Purity ≥98%
Appearance White to off-white solid.
Solubility Soluble in DMSO, DMF, ethanol or water.
InChi Key FSASIHFSFGAIJM-UHFFFAOYSA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Product Description

  • Potent cell permeable and selective inhibitor of phosphatidyl-inositol 3-kinase (PI3K) [1, 7, 8].
  • Blocks class I, class II and class III PI3Ks, including some downstream targets [8].
  • Blocks class I PI3K persistently and class III PI3K transiently [7].
  • Induces autophagy under nutrient-rich conditions and inhibits starvation-induced autophagy due to differential effects on class I versus class III PI3 kinase [5, 7].
  • Shows some limited Vps34 preference in vitro compared to PtdIns3Kγ. However, it is typically employed in cellular studies at a concentration of 10 mM, which can inhibit all PtdIns3Ks [8].
  • Can target other kinases and affect other cellular processes, such as glycogen metabolism, lysosomal acidification, endocytosis and mitochondrial permeability transition [2-4].
  • Anticancer compound [6, 10, 12].
  • Neuroprotective [9, 11].
  • PKA-activation dependent lipolytic agent. Enhances ATGL-dependent hydrolysis of triacylglycerols [13].

Product References

  1. 3-Methyladenine: specific inhibitor of autophagic/lysosomal protein degradation in isolated rat hepatocytes: P.O. Seglen & P.B. Gordon; PNAS 79, 1889 (1982)
  2. 3-Methyladenine, an inhibitor of autophagy, has multiple effects on metabolism: L.H. Caro, et al.; Eur. J. Biochem. 175, 325 (1988)
  3. 3-Methyladenine inhibits transport from late endosomes to lysosomes in cultured rat and mouse fibroblasts: E.L. Punnonen, et al.; Eur. J. Cell Biol. 65, 14 (1994)
  4. Inhibition of mitochondrial permeability transition and release of cytochrome c by anti-apoptotic nucleoside analogues: L. Xue, et al.; Biochem. Pharmacol. 64, 441 (2002)
  5. 3-methyladenine inhibits autophagy in tobacco culture cells under sucrose starvation conditions: C. Takatsuka, et al.; Plant Cell Physiol. 45, 265 (2004)
  6. 3-Methyladenine suppresses cell migration and invasion of HT1080 fibrosarcoma cells through inhibiting phosphoinositide 3-kinases independently of autophagy inhibition: S. Ito, et al.; Int. J. Oncol. 31, 261 (2007)
  7. Dual role of 3-methyladenine in modulation of autophagy via different temporal patterns of inhibition on class I and III phosphoinositide 3-kinase: Y.T. Wu, et al.; J. Biol. Chem. 285, 10850 (2010)
  8. Finding a fitting shoe for Cinderella: searching for an autophagy inhibitor: S. Miller, et al.; Autophagy 6, 805 (2010)
  9. Severe global cerebral ischemia-induced programmed necrosis of hippocampal CA1 neurons in rat is prevented by 3-methyladenine: a widely used inhibitor of autophagy: J.Y. Wang, et al.; J. Neuropathol. Exp. Neurol. 70, 314 (2011)
  10. Inhibitors of phosphatidylinositol 3'-kinases promote mitotic cell death in HeLa cells: H. Hou, et al.; PLoS One 7, e35665 (2012)
  11. Autophagy activation is associated with neuroprotection against apoptosis via a mitochondrial pathway in a rat model of subarachnoid hemorrhage: C.H. Jing, et al.; Neuroscience 213, 144 (2012)
  12. 3-Methyladenine induces cell death and its interaction with chemotherapeutic drugs is independent of autophagy: Y. Sheng, et al.; BBRC 432, 5 (2013)
  13. The autophagic inhibitor 3-methyladenine potently stimulates PKA-dependent lipolysis in adipocytes: B.L. Heckmann, et al.; Br. J. Pharmacol. 168, 163 (2013)
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