Lovastatin

製品コードS2061 バッチS206105

印刷

化学情報

 Chemical Structure Synonyms Mevinolin, MK-803 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C24H36O5

分子量 404.54 CAS No. 75330-75-5
Solubility (25°C)* 体外 DMSO 81 mg/mL (200.22 mM)
Ethanol 29 mg/mL (71.68 mM)
Water Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM in a cell-free assay, used for lowering cholesterol (hypolipidemic agent). Lovastatin triggers autophagy.
in vitro

Lovastatin inhibits LPS- and cytokine-mediated production of NO and expression of iNOS in rat primary astrocytes. This compound inhibits LPS-induced expression of TNF-alpha, IL-1beta, and IL-6 in rat primary astrocytes, microglia, and macrophages. [1]

This chemical results in over 95% inhibition of DNA synthesis as measured by incorporation of [3H]thymidine into DNA. It synchronizes cells in the G1 and not in the G0 phase of the cell cycle. It has a similar growth-inhibitory activity against ras-dependent as well as ras-independent cell lines. [2]

This agent produces a profound reduction of apolipoprotein-B-containing lipoproteins, especially LDL cholesterol and, to a lesser extent, plasma triglyc- erides, and a small increase in HDL cholesterol. [3]

It arrests cells by inhibiting the proteasome, which results in the accumulation of p21 and p27, leading to G1 arrest. This compound is an inhibitor of hydroxymethyl glutaryl (HMG)-CoA reductase, the rate-limiting enzyme in cholesterol synthesis. It can be used to arrest cultured cells in the G1 phase of the cell cycle, resulting in the stabilization of the cyclin-dependent kinase inhibitors (CKIs) p21 and p27. [4]

This chemical (2-10 mM) arrests cells in G1 and also prolonged--or arrested a minor fraction of cells in--the G2 phase of the cell cycle in human bladder carcinoma T24 cell line expressing activated p21ras. It (50 mM) is cytotoxic in human bladder carcinoma T24 cell line expressing activated p21ras. [5]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Astrocytes
濃度 10 μM
反応時間 8 h
実験の流れ

Cells preincubated in serum-free media with 10 µM lovastatin or 5 mM NaPA, or a combination of 2 µM this compound and 2 mM NaPA for 8 h received 1 µg/ml of LPS.

動物実験 動物モデル Male BALB/c athymic mice
投薬量 100 mg/kg
投与方法 o.g.

参考

  • https://pubmed.ncbi.nlm.nih.gov/9389730/
  • https://pubmed.ncbi.nlm.nih.gov/1711413/
  • https://pubmed.ncbi.nlm.nih.gov/12815379/
  • https://pubmed.ncbi.nlm.nih.gov/10393901/
  • https://pubmed.ncbi.nlm.nih.gov/1673788/
  • https://pubmed.ncbi.nlm.nih.gov/31037159/

カスタマーフィードバック

, , Clin Cancer Res, 2016, 22(13):3310-3319

Data from [Data independently produced by , , Cell Cycle, 2018, 17(9):1138-1145]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Coenzyme A protects against ferroptosis via CoAlation of mitochondrial thioredoxin reductase [ J Clin Invest, 2025, e190215] PubMed: 40694424
Dysregulated lipids homeostasis disrupts CHAC1-mediated ferroptosis driving fibroblast growth factor receptor tyrosine kinase inhibitor AZD4547 resistance in gastric cancer [ Redox Biol, 2025, 84:103693] PubMed: 40460553
African swine fever virus pB318L suppresses inflammatory response by inhibiting NF-κB activation and NLRP3 inflammasome formation [ PLoS Pathog, 2025, 21(10):e1013558] PubMed: 41124215
Lovastatin and Resveratrol Synergistically Improve Wound Healing and Inhibit Bacterial Growth [ Int J Mol Sci, 2025, 26(2)851] PubMed: 39859566
Pipeline to evaluate YAP-TEAD inhibitors indicates TEAD inhibition represses NF2-mutant mesothelioma [ Life Sci Alliance, 2025, 8(10)e202503241] PubMed: 40744733
Ferroptosis as a therapeutic vulnerability in MDM2 inhibition in dedifferentiated liposarcoma [ Oncol Lett, 2025, 29(6):269] PubMed: 40247991
Cholesterol Accumulation Enhances Cigarette Smoke-Induced Airway Epithelial Inflammation [ Int J Chron Obstruct Pulmon Dis, 2025, 20:411-423] PubMed: 40008109
Integration of 3D bioprinting and multi-algorithm machine learning identified glioma susceptibilities and microenvironment characteristics [ Cell Discov, 2024, 10(1):39] PubMed: 38594259
Multi-omics and pharmacological characterization of patient-derived glioma cell lines [ Nat Commun, 2024, 15(1):6740] PubMed: 39112531
Dysregulated Ribosome Biogenesis Is a Targetable Vulnerability in Triple-Negative Breast Cancer: MRPS27 as a Key Mediator of the Stemness-inhibitory Effect of Lovastatin [ Int J Biol Sci, 2024, 20(6):2130-2148] PubMed: 38617541

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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