MHY1485 是一种 mTOR 激活剂。它通过抑制自噬体和溶酶体之间的融合来抑制自噬过程,导致 LC3II 蛋白的积累和自噬体增大。
产品描述
MHY1485 is a mTOR activator. It inhibits the autophagic process by inhibition of fusion between autophagosomes and lysosomes, leading to the accumulation of LC3II protein and enlarged autophagosomes.
体内活性
MHY1485增加磷酸化mTOR水平和下游S6K1和rpS6蛋白的磷酸化,而不影响总mTOR含量,总S6K1和rpS6水平。卵巢经MHY1485短期处理后进行异种移植,可促进次级毛囊生长。MHY1485处理后进行移植,可促进成熟卵母细胞的生成,并产生健康后代。MHY1485以剂量和时间依赖性方式引起LC3II的聚集和自噬体的扩大。
激酶实验
Ovaries from mice at day10 of age are treated with 10 μM MHY1485 for 3h and proteins are extracted using M-PER Mammalian Protein Extraction Reagent containing a protease inhibitor cocktail. Protein concentrations in supernatants are determined by the bicinchoninic acid method. Equal amounts of protein lysates are loaded on 4-12% NuPAGE Bis-Tris gels in MOPS buffer and transferred to 0.45 μM pore nitrocellulose membranes[2].
细胞实验
MHY1485 is dissolved in DMSO and then diluted with appropriate media[3]. MC3T3-E1 cells are maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum (FBS), 100 U/mL penicillin and 100 mg/mL streptomycin at 37°C in a humidified atmosphere of 5% CO2. Having reached 70% confluence, the culture medium is switched to commercial osteogenic differentiation medium. MC3T3-E1 cells are cultured in the osteogenic differentiation medium for 14 days, following by culture in DMEM supplemented with varying concentrations of liraglutide (catalog no. HY-P0014; MedChem Express) for a further 14 days. MC3T3-E1 cells treated with 4 nM liraglutide are cultured in the presence or absence of Compound C or MHY1485. MC3T3-E1 cells maintained in DMEM for 28 days in the absence of any treatment are used as the negative control (NC); cells cultured in commercial osteogenic differentiation medium for 14 days and in DMEM without liraglutide for an additional 14 days are used as the positive control (PC)[3].
Cas No.
326914-06-1
分子式
C17H21N7O4
分子量
387.4
储存和溶解度
Ethanol:<1 mgml
H2O:<1 mgml
DMSO:9 mg/mL(23.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years