3-Methyladenine
3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. 3-Methyladenine (3-MA) is successfully used to suppress mitophagy.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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Autophagy,2010 Aug;6(6):805-7.
Finding a fitting shoe for Cinderella: searching for an autophagy inhibitor.[Pubmed:
20574157]
Vps34 is the ancestral phosphatidylinositol 3-kinase (PtdIns3K) isoform and is essential for endosomal trafficking of proteins to the vacuole/lysosome, autophagy and phagocytosis. Vps34-containing complexes associate with specific cellular compartments to produce PtdIns(3)P. Understanding the roles of Vps34 has been hampered by the lack of potent, specific inhibitors.
METHODS AND RESULTS:
To boost development of Vps34 inhibitors, we determined the crystal structures of Vps34 alone and in complexes with multitargeted PtdIns3K inhibitors. These structures provided a first glimpse into the uniquely constricted ATP-binding site of Vps34 and enabled us to model Vps34 regulation. We showed that the substrate-binding "activation" loop and the flexibly attached amphipathic C-terminal helix are crucial for catalysis on membranes. The C-terminal helix also suppresses ATP hydrolysis in the absence of membranes.
CONCLUSIONS:
We propose that membrane binding shifts the C-terminal helix to orient the enzyme for catalysis, and the Vps15 regulatory subunit, which binds to this and the preceding helix, may facilitate this process. This C-terminal region may also represent a target for specific, non-ATP-competitive PtdIns3K inhibitors.
J Biol Chem,2010 Apr 2;285(14):10850-61.
Dual role of 3-methyladenine in modulation of autophagy via different temporal patterns of inhibition on class I and III phosphoinositide 3-kinase.[Pubmed:
20123989]
HeLa cells are radiolabeled for 24 hours with 0.05 mCi/mL l-[U- 14C]valine. At the end of the labeling period, cells are rinsed three times with PBS. Cells are incubated for the designated times in either full medium or EBSS with or without the presence of 10 mM 3-Methyladenine.
PLoS One,2012;7(4):e35665.
Inhibitors of phosphatidylinositol 3'-kinases promote mitotic cell death in HeLa cells.[Pubmed:
22545128]
Cell lines:HeLa cell line
Concentrations: 1-10 mM
Incubation Time: 24, 48 or 72 hours
Method:
Cell (such as HeLa cell) viability is determined by a trypan blue exclusion assay. Briefly, after treated with 3-Methyladenine, both adherent and floating cells are collected and suspended in phosphate buffered saline (PBS, pH 7.4) at a final density of 1-2 × 106/mL. An equal volume of 0.4% trypan blue solution (w/v, in PBS) is added to the cell suspension and mixed thoroughly. After incubation at room temperature for 3 min, cell counting is performed using a hemacytometer.
Neuroscience,2012 Jun 28;213:144-53.
Autophagy activation is associated with neuroprotection against apoptosis via a mitochondrial pathway in a rat model of subarachnoid hemorrhage.[Pubmed:
22521819]
Animal Models: Adult male Sprague–Dawley rats weighing 300-350 g
Dosages: 400 nM
Administration: Intracerebral ventricular
