MW 432.4 Da, Purity >98%. Potent, selective, ATP-competitive mTOR inhibitor. Inhibits mTORC1 (IC50 = 2.1 nM) in in vitro kinase activity assays. Displays 800-fold selectivity for mTOR over PI3K (cellular EC50 values are 0.25 and 200 nM for mTOR and PI3K respectively). Attenuates phosphorylation of mTOR downstream targets, inhibits cell proliferation of several cancer cell types, and induces apoptosis and autophagy. Also exhibits potent biochemical and cellular activity against phosphatidylinositol-3 kinase-like kinase (PIKK) family kinases including ATM, ATR and DNA-PK (EC50 values are 28 nM, 35 nM and 118 nM respectively). Has significantly improved bioavailability (54%), metabolic stability, and plasma exposure compared to Torin 1 (ab218606).
View Alternative Names
FK506 binding protein 12 rapamycin associated protein 1, FK506 binding protein 12 rapamycin associated protein 2, FK506-binding protein 12-rapamycin complex-associated protein 1, FKBP rapamycin associated protein, FKBP12-rapamycin complex-associated protein, FKBP12-rapamycin complex-associated protein 1, FLJ44809, FRAP, FRAP1, FRAP2, MTOR_HUMAN, Mammalian target of rapamycin, Mechanistic target of rapamycin, OTTHUMP00000001983, RAFT1, RAPT1, Rapamycin and FKBP12 target 1, Rapamycin associated protein FRAP2, Rapamycin target protein, Rapamycin target protein 1, Serine/threonine-protein kinase mTOR, dJ576K7.1 (FK506 binding protein 12 rapamycin associated protein 1)
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Appropriate long-term storage conditions
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Supplementary information
This supplementary information is collated from multiple sources and compiled automatically.
Biological function summary
MTOR integrates signals from nutrients growth factors and cellular energy status to maintain cellular homeostasis. It forms part of two distinct complexes mTORC1 and mTORC2 which differ in their component proteins and downstream effects. mTORC1 primarily responds to amino acids and regulates protein synthesis through phosphorylation of key substrates like S6K1. On the other hand mTORC2 is important for maintaining cytoskeletal integrity and cell survival highlighting the protein's importance in diverse cellular processes.
Pathways
MTOR plays a pivotal role in the PI3K/AKT/mTOR pathway which governs cell growth proliferation and survival. It also has implications in the regulation of the AMPK pathway which senses cellular energy levels. Through these pathways mTOR interacts with proteins such as AKT and TSC2. The phospho-mTOR specifically the S2448 phospho-mTOR serves as an important functional marker in these signaling cascades linking extracellular signals to downstream cellular responses.
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