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Mevastatin

MCE China：Mevastatin

Brand：MedChemExpress (MCE)

Cat. No.HY-17408

CAS：73573-88-3

Synonyms：Compactin; ML236B

Purity：99.46%

Storage：4°C, protect from light *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment.

In Vitro：Mevastatin (0-128 μM; 5 days; Caco-2 cells) treatment causes a dose-dependent decrease in cell number[1]. Mevastatin (32-128 μM; 24-72 hours; Caco-2 cells) treatment causes an early G0/G1 phase and a late G2/M phase cell cyclr arrest[1]. Mevastatin (32-128 μM; 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[1]. Mevastatin (16-256 μM; Caco-2 cells) treatment induces apoptosis in a dose-dependent manner[1]. 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[4].

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[2]. 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[3].

IC50 & Target：HMG-CoA reductase[1][2] Apoptosis[1] Cellular Effect Cell Line Type Value Description References

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References：

[1]. Wächtershäuser A, et al. HMG-CoA reductase inhibitor mevastatin enhances the growth inhibitory effect of butyrate in the colorectal carcinoma cell line Caco-2. Carcinogenesis. 2001 Jul;22(7):1061-7.  [Content Brief]

[2]. Amin-Hanjani S, Stagliano NE, Yamada M, et al. Mevastatin, an HMG-CoA reductase inhibitor, reduces stroke damage and upregulates endothelial nitric oxide synthase in mice. Stroke. 2001 Apr;32(4):980-6.  [Content Brief]

[3]. Sugazaki M, Hirotani H, Echigo S, et al. Effects of mevastatin on grafted bone in MRL/MpJ mice. Connect Tissue Res. 2010 Apr;51(2):105-12.  [Content Brief]

[4]. Evangelopoulos ME, Weis J, Krüttgen A. Mevastatin-induced neurite outgrowth of neuroblastoma cells via activation of EGFR. J Neurosci Res. 2009 Jul;87(9):2138-44.  [Content Brief]