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.
Life Sci. 2020 Jun 15;251:117595.
The in vitro effects of phospholipase D1-mTOR axis in liver fibrogenesis
MHY1485 purchased from AbMole
Fish Shellfish Immunol. 2020 Jul;102:480-488.
Target of rapamycin signaling inhibits autophagy in sea cucumber Apostichopus japonicus
MHY1485 purchased from AbMole
|Source||Life Sciences (2020 Jun). Figure 5. MHY1485 (Abmole Bioscience, US)|
|Method||Proliferation analysis by CCK-8 method|
|Cell Lines||Rat HSCs cell line|
|Incubation Time||48 h|
|Results||Moreover, both PLD1-I and PLD1-SiRNA could significantly blunt proliferation of HSC-T6 treated with MHY1485 (mTOR activator)|
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO 7 mg/mL (Need ultrasonic and warming)|
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