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|Solubility (25°C) *||In vitro||DMSO||4 mg/mL (10.32 mM)|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Description||MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.|
|In vitro||MHY1485 suppresses the basal autophagic flux. MHY1485 causes the accumulation of LC3II and enlargement of the autophagosomes in a dose- and time- dependent manner. MHY1485 increases phospho-mTOR levels and phosphorylation of downstream S6K1 and rpS6 proteins without affecting total mTOR content, total S6K1 and rpS6 levels. Short-term treatment of ovaries with MHY1485 followed by allo-transplantation promoted secondary follicle growth. Treatment with MHY1485 and subsequent grafting allowed the derivation of mature oocytes and healthy offspring.|
|Activation of mTOR||Western blot analysis is performed to detect the change of total protein level and levels of phosphorylated forms of mTOR and 4E-BP1 reflecting the activity of mTOR. Ac2F cells are treated with MHY1485 of different concentrations and rapamycin 5 mM as a positive control for 1 h. Cells are washed with cold PBS and harvested. Cell lysates are prepared using RIPA buffer (50 mM Tris-HCl, 150 mM NaCl, 1% NP-40, 1 mM DTT, 0.1 mM NaF, 1 mM PMSF, 1 mg/mL pepstatin, 1 mg/mL leupeptin, and 1 mg/mL aprotinin). Protein concentration is determined by the bicinchoninic acid (BCA) method. Equal amounts of protein are separated on 10-12% sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) gels. The gels are subsequently transferred onto a polyvinylidene difluoride membrane by electroblotting for 2 h at 60-75 V. The membranes are blocked in a 5% nonfat milk solution in Tris-buffered saline (TBS) with 0.5% Tween-20, and incubated with primary antibodies. Pre-stained protein markers are used for molecular-weight determination.|
Data from [Data independently produced by , , Biochem J, 2017, 474(16):2733-2747]
MYH1485, an activator of mTOR, reduced LC3II production and inhibited autophagosome formation in PAR2-knockdown cells.
Data from [Data independently produced by , , Mol Med Rep, 2016, 14(4):3662-8.]
Effects of liraglutide treatments and AMPK inhibitor/mTOR activator on matrix mineralization and relative protein levels of Alp, OC, p‑AMPK, p‑mTOR and TGF‑β. Following culture in commercial osteogenic differentiation medium for 14 days, MC3T3‑E1 cells were cultured for a further 14 days in basal culture medium with 4 nM liraglutide, and 4 nM liraglutide plus AMPK inhibitor, 10 μM compound C, or 1 μM mTOR activator, MHY1485. MC3T3‑E1 cells maintained in DMEM for 28 days with no treatment were used as the NC;cells cultured in the commercial osteogenic differentiation medium for 14 days and in DMEM without liraglutide for a further 14 days were used as the PC. (B) Relative protein expression was analyzed by western blot and quantifi ed relative to GAPDH (n=5). Data are presented as the mean ± standard error. Bars with letters means they signifi cantly differ with positive control (P<0.05). *P<0.05, **P<0.05 vs. NC; #P<0.05, ##P<0.01 vs. PC. NC, negative control; PC, positive control; Alp, alkaline phosphatase; OC, osteocalcin; p‑, phosphorylated; AMPK, adenosine monophosphate‑activated protein kinase; mTOR, mechanistic target of rapamycin; TGF‑β, transforming growth factor‑β; GAPDH, glyceraldehyde 3‑phosphate dehydrogenase.
Protease-activated receptor-2 promotes kidney tubular epithelial inflammation by inhibiting autophagy via the PI3K/Akt/mTOR signalling pathway. [Du C, et al. Biochem J, 2017, 474(16):2733-2747]PubMed: 28694352
Liraglutide attenuates the osteoblastic differentiation of MC3T3‑E1 cells by modulating AMPK/mTOR signaling. [Hu XK, et al. Mol Med Rep, 2016, 14(4):3662-8]PubMed: 27600753
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