PP242
Dual mTORC1/mTORC2 inhibitor / PP242 is an ATP-competitive mTORC1/mTORC2 inhibitor (IC50 = 8 nM) displaying high selectivity over PI 3K family kinases (IC50s =0.102 to 2.2 μM) and modest selectivity over PKC family kinases (IC50s =0.049 to 0.198 μM).1,2 PP 242 (but not rapamycin) induced the death of mouse and human leukemia cells but was much weaker than rapamycin at induction of death of normal lymphocytes.3 Restores lysosomal activity and facilitates clearance of amyloid-β in a mouse model of dry age-related macular degeneration.4 Inhibits glioblastoma cell proliferation, migration, invasiveness, and stemness.5
Biochemicals & reagents
1092351-67-1
Torkinib
1 Aspel et al. (2008), Targeted polypharmacology: Discovery of dual inhibitors of tyrosine and phosphoinositide kinases; Nat. Chem. Biol. 4 691 2 Feldman et al. (2009), Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2; PLoS Biol. 7 371 3 Janes et al. (2010), Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor; Nat. Med. 16 205 4 Jo et al. (2023), Activation of Lysosomal Function Ameliorates Amyloid-ß-Induced Tight Junction Disruption in the Retinal Pigment Epithelium; Mol. Cells 46 675 5 Mecca et al. (2018), PP242 Counteracts Glioblastoma Cell Proliferation, Migration, Invasiveness and Stemness Properties by Inhibiting mTORC2/AKT; Front. Cell. Neurosci. 12 99
-20°C
TARGET: Kinase; Lysosome -- PATHWAY: mTOR; Intracellular transport -- RESEARCH AREA: Neuroscience; Cancer stem cells -- DISEASE AREA: Cancer