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Mevastatin
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Mevastatin
CAS No. : 73573-88-3
MCE 站:Mevastatin
产品活性:Mevastatin (Compactin) 是个属于他汀类的 HMG-CoA 还原酶抑制剂。Mevastatin 是一种降脂药,可诱导细胞凋亡,将癌细胞阻滞在 G0/G1 期。Mevastatin 还可以增加内皮型一氧化氮合酶 (eNOS) 的 mRNA 和蛋白质水平。Mevastatin 具有抗肿瘤活性,并可用于心血管疾病的研究。
研究领域:Metabolic Enzyme/Protease | Anti-infection | Autophagy | Apoptosis
作用靶点:HMG-CoA Reductase (HMGCR) | Bacterial | Autophagy | Apoptosis | Antibiotic
In Vitro: Mevastatin (0-128 ?M; 5 days; Caco-2 cells) treatment causes a dose-dependent decrease in cell number.
Mevastatin (32-128 ?M; 24-72 hours; Caco-2 cells) treatment causes an early G0/G1 phase and a late G2/M phase cell cyclr arrest.
Mevastatin (32-128 ?M; 72 hours; Caco-2 cells) treatment causes a down-regulation of cyclin-dependent kinases (cdk) 4 and cdk 6 as well as cyclin D1, while cdk 2 and cyclin E protein levels remained unchanged. Cell cycle inhibitors p21 and p27 are significantly upregulated by Mevastatin.
Mevastatin (16-256 ?M; Caco-2 cells) treatment induces apoptosis in a dose-dependent manner.
Treatment of Neuro2a cells with mevastatin for 24 hours induced neurite outgrowth associated with up-regulation of the neuronal marker protein NeuN. Mevastatin triggers phosphorylation of the key kinases epidermal growth factor receptor (EGFR), ERK1/2, and Akt/protein kinase B. Inhibition of EGFR, PI3K, and the mitogen-activated protein kinase cascade blocks Mevastatin-induced neurite outgrowth.
In Vivo: Mevastatin (2-20 mg/kg; delivered via ALZET miniosmotic pumps; daily; for 7, 14, or 28 days; wild-type 129-SV/eVTAcBr male mice and eNOS-deficient male mice) treatment increases levels of endothelial nitric oxide synthase (eNOS) mRNA and protein, reduces infarct size, and improves neurological deficits in a dose- and time-dependent manner.
The topical infusion of Mevastatin (2.5 pmol/hr) increases bone mass (MRL/MpJ mouse) of isografted bone by increasing bone turnover and, at least in part, by promoting the expression of bone morphogenetic protein-2 (BMP-2) mRNA and receptor activator of NF-κB ligand (RANKL) mRNA.
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热门标签:Compactin