MHY1485 induced mTOR activation and correspondingly showed a higher docking score than PP242, a well-known ATP-competitive mTOR inhibitor, in docking simulation. In conclusion, MHY1485 has an inhibitory effect on the autophagic process by inhibition of fusion between autophagosomes and lysosomes leading to the accumulation of LC3II protein and enlarged autophagosomes. MHY1485 also induces mTOR activity, providing a possibility for another regulatory mechanism of autophagy by the MHY compound. MHY1485 treatment increases ribosomal protein S6 kinase (S6K) and eukaryotic translation initiation factor 4E-binding protein 1 (4E-BP1) phosphorylation, which are downstream targets of mTOR complex 1 (mTORC1), but decreases phosphorylation of Akt on mTOR complex 2 (mTORC2) target site serine 473.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 7 mg/mL (Need ultrasonic and warming)|
Promotion of ovarian follicle growth following mTOR activation: synergistic effects of AKT stimulators.
Cheng Y, et al. PLoS One. 2015 Feb 24;10(2):e0117769. PMID: 25710488.
Inhibitory effect of mTOR activator MHY1485 on autophagy: suppression of lysosomal fusion.
Choi YJ, et al. PLoS One. 2012;7(8):e43418. PMID: 22927967.
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