The PI3K/Akt/mTOR signaling pathway is a key regulator in growth, survival, cell cycle proliferation, protein synthesis and glucose metabolism. Growth factors, hormones, and cytokines can activate this pathway by binding their cognate receptor tyrosine kinase (RTK), cytokine receptor, or GPCR, resulting in the activation of lipid kinase PI3K which produces PIP3 at the plasma membrane.
The binding of PIP3 translocates Akt to cell membranes, enables Akt activation through phosphorylation at Thr308 mediated by phosphoinositide dependent kinase 1 (PDK1). In addition, Akt is phosphorylated at Ser473 by the mTOR-rictor complex, mTORC2. PTEN is a negative regulator of Akt signaling that reverses the function of PI3K by removing 3’-phosphate groups. Akt activity is also negatively regulated by the phosphatases PP2A and PHLPP. Akt propagates its signal to affect DNA transcription, cell cycle and apoptosis. Akt can activate mTOR directly by phosphorylation or indirectly, by phosphorylation and inactivation of mTOR inhibitor TSC2 and PRAS40. Together these mechanisms stimulate cell growth and G1 cell cycle progression through signaling via p70 S6 Kinase and inhibition of 4E-BP1. Defects in PI3K/AKT/mTOR signaling are implicated in cancer, diabetes and cardiovascular disease etc.
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- 740 Y-PCatalog No. :B5246PI 3-kinase activator,cell permeable
740 Y-P is an activator of PI3K with concentration of 20 μM .
- PI-3065Catalog No. :B4660P110δkinase inhibitorPI-3065 is a small molecule and selective inhibitor of p110δkinase with an Ki value of 1.5nM and IC50 value of 5nM .
- WZ4003Catalog No. :B1374NUAK1/2 inhibitor, potent and selectiveWZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively, without significant inhibition on 139 other kinases.
- Niclosamide Ethanolamine saltCatalog No. :B8383An anthelmintic originally, mitochondrial uncoupler in parasitic worms and other animals, also used in prevention and treatment of obesity and type 2 diabetes
- Akt Inhibitor IVCatalog No. :C5867
- Rapalink-1Catalog No. :A8764third-generation mTOR inhibitor
- GDC-0084Catalog No. :B7826PI3K and mTOR inhibitor, brain-permeableGDC-0084 is a potent and brain penetrant inhibitor of PI3K and mTOR with Ki values of 2 nM and 70 nM for PI3Kα and mTOR, respectively .
- 3-Guanidinopropionic AcidCatalog No. :C5645AMPK stimulator
- NG,NG-dimethyl-L-Arginine (hydrochloride)Catalog No. :C5216endogenous nitric oxide synthase inhibitor
- KP372-1Catalog No. :C5053specific Akt inhibitor