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Simvastatin

Catalog No. T0687 CAS 79902-63-9

Synonyms: MK-0733, MK 733

Simvastatin (MK 733) is an HMG-CoA reductase inhibitor (Ki=0.2 nM) with oral activity. Simvastatin has hypolipidemic activity, inhibits hepatic production of cholesterol, and is also used for the prevention of cardiovascular disease.

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Simvastatin, CAS 79902-63-9

Pack Size	Availability	Price/USD
10 mg	In stock	$ 36.00
25 mg	In stock	$ 53.00
50 mg	In stock	$ 63.00
100 mg	In stock	$ 108.00
200 mg	In stock	$ 30.00
500 mg	In stock	$ 46.00
1 g	In stock	$ 64.00
5 g	In stock	$ 148.00
1 mL * 10 mM (in DMSO)	In stock	$ 39.00

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Purity: 99.95%

Purity: 98.54%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Simvastatin (MK 733) is an HMG-CoA reductase inhibitor (Ki=0.2 nM) with oral activity. Simvastatin has hypolipidemic activity, inhibits hepatic production of cholesterol, and is also used for the prevention of cardiovascular disease.
Targets&IC50	HMG-CoA reductase:0.1-0.2 nM(Ki)
In vitro	METHODS: BCa cells 5637, EJ and T24 were treated with Simvastatin (0.5-40 µM) for 48 h. Cell viability was measured by MTT assay. RESULTS: Simvastatin significantly inhibited the survival of the three BCa cells in a dose-dependent manner. [1] METHODS: Human fibroblast SAEC and four tumor cells MCF7, HepG2, NCH, NCI were treated with Simvastatin (20 µM) for 72 h. Apoptosis was detected by TUNEL. RESULTS: Simvastatin induced apoptosis in different types of human tumor cells, but not in SAEC cells. [2]
In vivo	METHODS: To study in vivo activity, Simvastatin (60 mg/kg, aqueous 2% DMSO+30% PEG 400+5% Tween 80) was administered by gavage to C57BL/6J mice once daily for six weeks on a CF diet. RESULTS: Simvastatin treatment reduced serum cholesterol levels by 18%, and retinal cholesterol and lipoprotein cholesterol levels by 24% and 21%, respectively. [3] METHODS: To assay antitumor activity in vivo, Simvastatin (5-50 mg/kg in methylcellulose) was administered to BALB/c nu/nu mice by gavage once daily for three days. Subsequently, colorectal cancer cells COLO205 were subcutaneously inoculated into the right side of the mice. RESULTS: Simvastatin inhibited tumor growth in a xenograft mouse model by inducing tumor cell apoptosis and inhibiting tumor angiogenesis. [4]
Kinase Assay	For assessment of Akt protein kinase activity in vitro, substrate (2 μg histone H2B or 25 μg eNOS peptide) is incubated with Akt immunoprecipitated from cell lysate using goat polyclonal anti-Akt1 antibody. Kinase reactions are initiated following the addition of reaction components to a final concentration of ATP (50 μM) containing 10 μCi of 32P-γATP, dithiotreitol (1 mM), HEPES buffer (20 mM, pH 7.4), MnCl2 (10 mM), MgCl2 (10 mM). After incubation for 30 min at 30°C, phosphorylated histone H2B is visualized after SDS-PAGE (15%) and autoradiography. To estimate the extent of 32P incorporation into eNOS peptides, each reaction mixture is measured by spotting onto phosphocellulose disc filter and the amount of phosphate incorporated is measured by Cerenkov counting. The wild-type peptide sequence is 1174-RIRTQSFSLQERHLRGAVPWA-1194, and the mutant eNOS peptide is identical except that serine 1179 is substituted by alanine.

Synonyms	MK-0733, MK 733
Molecular Weight	418.57
Formula	C25H38O5
CAS No.	79902-63-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 31.4 mg/mL (75 mM)

DMSO: 50 mg/mL (119.45 mM)

References and Literature

1. Wang G, et al. Simvastatin induces cell cycle arrest and inhibits proliferation of bladder cancer cells via PPARγ signalling pathway. Sci Rep. 2016 Oct 25;6:35783. 2. Spampanato C, et al. Simvastatin inhibits cancer cell growth by inducing apoptosis correlated to activation of Bax and down-regulation of BCL-2 gene expression. Int J Oncol. 2012 Apr;40(4):935-41. 3. Mast N, et al. Retinal Cholesterol Content Is Reduced in Simvastatin-Treated Mice Due to Inhibited Local Biosynthesis Albeit Increased Uptake of Serum Cholesterol. Drug Metab Dispos. 2018 Nov;46(11):1528-1537. 4. Cho SJ, et al. Simvastatin induces apoptosis in human colon cancer cells and in tumor xenografts, and attenuates colitis-associated colon cancer in mice. Int J Cancer. 2008 Aug 15;123(4):951-7. 5. Ishida F, et al. Biochim Biophys Acta, 1990, 1042(3), 365-373. 6. Liu Z, et al. Pretreatment Donors after Circulatory Death with Simvastatin Alleviates Liver Ischemia Reperfusion Injury through a KLF2-Dependent Mechanism in Rat. Oxid Med Cell Longev. 2017;2017:3861914. 7. Wei Y H, Liao S L, Wang S H, et al. Simvastatin and ROCK Inhibitor Y-27632 Inhibit Myofibroblast Differentiation of Graves’ Ophthalmopathy-Derived Orbital Fibroblasts via RhoA-Mediated ERK and p38 Signaling Pathways[J]. Frontiers in Endocrinology. 2021, 11: 1109. 8. Wei Y H, Liao S L, Wang C C, et al. Simvastatin Inhibits CYR61 Expression in Orbital Fibroblasts in Graves’ Ophthalmopathy through the Regulation of FoxO3a Signaling[J]. Mediators of Inflammation. 2021, 2021. 9. Tang Y, Fang G, Guo F, et al. Selective Inhibition of STRN3-Containing PP2A Phosphatase Restores Hippo Tumor-Suppressor Activity in Gastric Cancer[J]. Cancer Cell. 2020, 38(1): 115-128. e9.

Citations

1. Zhang W, Pan X, Xu Y, et al.Mevalonate improves anti-PD-1/PD-L1 efficacy by stabilizing CD274 mRNA.Acta Pharmaceutica Sinica B.2023 2. Wang D, Wang Y, Di X, et al.Cortical tension drug screen links mitotic spindle integrity to Rho pathway.Current Biology.2023 3. Zhang L, Yi Y, Wang T, et al.25-Hydroxycholesterol inhibits classical swine fever virus entry into porcine alveolar macrophages by depleting plasma membrane cholesterol.Veterinary Microbiology.2023: 109668. 4. Wei Y H, Liao S L, Wang S H, et al. Simvastatin and ROCK Inhibitor Y-27632 Inhibit Myofibroblast Differentiation of Graves’ Ophthalmopathy-Derived Orbital Fibroblasts via RhoA-Mediated ERK and p38 Signaling Pathways. Frontiers in Endocrinology. 2021 Feb 1;11:607968. doi: 10.3389/fendo.2020.607968. eCollection 2020. 5. Wei Y H, Liao S L, Wang C C, et al. Simvastatin Inhibits CYR61 Expression in Orbital Fibroblasts in Graves’ Ophthalmopathy through the Regulation of FoxO3a Signaling. Mediators of Inflammation. 2021 Jan 20;2021:8888913. doi: 10.1155/2021/8888913. eCollection 2021. 6. Tang Y, Fang G, Guo F, et al. Selective Inhibition of STRN3-Containing PP2A Phosphatase Restores Hippo Tumor-Suppressor Activity in Gastric Cancer. Cancer Cell. 2020, 38(1): 115-128. e9. 7. Khalifa B A, Guijarro A, Ravera S, et al.Cyclic fasting bolsters cholesterol biosynthesis inhibitors’ anticancer activity.Nature Communications.2023, 14(1): 6951. 8. Noè R, Inglese N, Romani P, et al.Organic Selenium induces ferroptosis in pancreatic cancer cells.Redox Biology.2023: 102962. 9. Tan X D, Luo C F, Liang S Y.Antihyperlipidemic drug rosuvastatin suppressed tumor progression and potentiated chemosensitivity by downregulating CCNA2 in lung adenocarcinoma.Journal of Chemotherapy.2024: 1-13.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Microbial Natural Product Library Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Inhibitor Library FDA-Approved & Pharmacopeia Drug Library Clinical Compound Library

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Keywords

Simvastatin 79902-63-9 Apoptosis Autophagy Metabolism Ferroptosis Mitophagy HMG-CoA Reductase HMG-CoA Reductase (HMGCR) Huh7 HepG2 anticancer MK733 MK-733 Inhibitor inhibit MK-0733 oral activity MK0733 MK 0733 MK 733 anti-proliferation activity cholesterol synthesis Mitochondrial Autophagy inhibitor

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