MHY1485 - mTOR Activator - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMHY1485Cat. No.: HY-B0795CAS No.: 326914-06-1分式: CHNO分量: 387.39作靶點(diǎn): mTOR; Autophagy作通路: PI3K/Akt/mTOR; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 9.5 mg/mL (24.52 mM; Need ult

2、rasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.5814 mL 12.9069 mL 25.8138 mL5 mM 0.5163 mL 2.5814 mL 5.1628 mL10 mM 0.2581 mL 1.2907 mL 2.5814 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 MHY1485可滲透細(xì)胞的 mTOR 活化劑。 MHY1485通過(guò)抑制噬體和溶酶體之間的融合抑制噬過(guò)程。IC50 & Tar

3、get mTORC1 mTORC2 Autophagy體外研究MHY1485 induces mTOR activity, which is another regulator of autophagy. MHY1485 markedly increasesthe LC3II/LC3I ratio dose-dependently and time-dependently 1. An mTOR activator MHY1485 stimulatesmTOR, S6K1 and rpS6 phosphorylation. Treatment with MHY1485 increases pho

4、spho-mTOR levels without1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEaffecting total mTOR content. MHY1485 treatment also increases the phosphorylation of downstream S6K1and rpS6 proteins without affecting total S6K1 and rpS6 levels 2. An mTOR activator, MHY1485, alsoabolishes the inhibitory eff

5、ect of liraglutide on osteoblastic differentiation, and results in p-mTOR and TGF-downregulation, but does not attenuate the liraglutide-induced increase in p-AMPK protein expression levels.Co-treatment with 4 nM Liraglutide and 1 M MHY1485, an mTOR activator, results in protein expressionlevels of

6、Alp, OC, p-mTOR and TGF- and matrix mineralization comparable to those of positive control cellscells 3. MHY1485 treatment increases ribosomal protein S6 kinase (S6K) and eukaryotic translationinitiation factor 4E-binding protein 1 (4E-BP1) phosphorylation, which are downstream targets of mTORcomple

7、x 1 (mTORC1), but decreases phosphorylation of Akt on mTOR complex 2 (mTORC2) target siteserine 473 4.PROTOCOLKinase Assay 2 Ovaries from mice at day10 of age are treated with 10 M MHY1485 for 3h and proteins are extracted usingM-PER Mammalian Protein Extraction Reagent containing a protease inhibit

8、or cocktail. Proteinconcentrations in supernatants are determined by the bicinchoninic acid method. Equal amounts of proteinlysates are loaded on 4-12% NuPAGE Bis-Tris gels in MOPS buffer and transferred to 0.45 M porenitrocellulose membranes 2.MCE has not independently confirmed the accuracy of the

9、se methods. They are for reference only.Cell Assay 3 MC3T3-E1 cells are maintained in Dulbeccos modified Eagles medium (DMEM) supplemented with 10%fetal bovine serum (FBS), 100 U/mL penicillin and 100 mg/mL streptomycin at 37C in a humidifiedatmosphere of 5% CO2. Having reached 70% confluence, the c

10、ulture medium is switched to commercialosteogenic differentiation medium. MC3T3-E1 cells are cultured in the osteogenic differentiation medium for14 days, following by culture in DMEM supplemented with varying concentrations of liraglutide (catalog no.HY-P0014; MedChem Express) for a further 14 days

11、. MC3T3-E1 cells treated with 4 nM liraglutide arecultured in the presence or absence of Compound C or MHY1485. MC3T3-E1 cells maintained in DMEM for28 days in the absence of any treatment are used as the negative control (NC); cells cultured in commercialosteogenic differentiation medium for 14 day

12、s and in DMEM without liraglutide for an additional 14 days areused as the positive control (PC) 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Death Dis. 2019 Feb 13;10(2):140. J Infect. 2019 Jun 18. pii: S0163-4453(19)30187-2. Bioc

13、hem Pharmacol. 2016 Dec 15;122:42-61. Respir Res. 2018 Dec 5;19(1):243. Life Sci. 2019 May 1;224:95-108.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Choi YJ, et al. Inhibitory effect of mTOR activator MHY1485 on autophagy: sup

14、pression of lysosomal fusion. PLoS One.2012;7(8):e43418.2. Cheng Y, et al. Promotion of Ovarian Follicle Growth following mTOR Activation: Synergistic Effects of AKT Stimulators. PLoS One.2015 Feb 24;10(2):e0117769.3. Hu XK, et al. Liraglutide attenuates the osteoblastic differentiation of MC3T3 E1 cells by modulating AMPK/mTOR signaling. Mol MedRep. 2016 Oct;14(4):3662-8.4. Rakhmanova V, et al. Inhibition of Mast Cell Function and Proliferation by mTOR Activator MHY1485. Immune Netw. 2