Lovastatin

製品コードS2061 バッチS206104

化学情報

	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	80 mg/mL (197.75 mM)
		Ethanol	35 mg/mL (86.51 mM)
		Water	Insoluble
* <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. Lovastatin inhibits LPS-induced expression of TNF-alpha, IL-1beta, and IL-6 in rat primary astrocytes, microglia, and macrophages. ^[1] Lovastatin results in over 95% inhibition of DNA synthesis as measured by incorporation of [3H]thymidine into DNA. Lovastatin synchronizes cells in the G1 and not in the G0 phase of the cell cycle. Lovastatin has a similar growth-inhibitory activity against ras-dependent as well as ras-independent cell lines. ^[2] Lovastatin 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] Lovastatin arrests cells by inhibiting the proteasome, which results in the accumulation of p21 and p27, leading to G1 arrest. Lovastatin is an inhibitor of hydroxymethyl glutaryl (HMG)-CoA reductase, the rate-limiting enzyme in cholesterol synthesis. Lovastatin 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] Lovastatin (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. Lovastatin (50 mM) is cytotoxic in human bladder carcinoma T24 cell line expressing activated p21ras. ^[5]

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. Lovastatin inhibits LPS-induced expression of TNF-alpha, IL-1beta, and IL-6 in rat primary astrocytes, microglia, and macrophages. ^[1]

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

Lovastatin 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]

Lovastatin arrests cells by inhibiting the proteasome, which results in the accumulation of p21 and p27, leading to G1 arrest. Lovastatin is an inhibitor of hydroxymethyl glutaryl (HMG)-CoA reductase, the rate-limiting enzyme in cholesterol synthesis. Lovastatin 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]

Lovastatin (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. Lovastatin (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 lovastatin 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

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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：

Integration of 3D bioprinting and multi-algorithm machine learning identified glioma susceptibilities and microenvironment characteristics [ Cell Discov, 2024, 10(1):39]	PubMed: 38594259
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
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
African swine fever virus pB318L, a trans-geranylgeranyl-diphosphate synthase, negatively regulates cGAS-STING and IFNAR-JAK-STAT signaling pathways [ PLoS Pathog, 2024, 20(4):e1012136]	PubMed: 38620034
Necrosulfonamide causes oxidation of PCM1 and impairs ciliogenesis and autophagy [ iScience, 2024, 27(4):109580]	PubMed: 38600973
Ku80 is indispensable for repairing DNA double-strand breaks at highly methylated sites in human HCT116 cells [ DNA Repair (Amst), 2024, 134:103627]	PubMed: 38219597
Cholesterol biosynthesis inhibition synergizes with AKT inhibitors in triple-negative breast cancer [ bioRxiv, 2024, 10.1101/2024.01.16.575899]	PubMed: none
NINJ1 regulates ferroptosis via xCT antiporter interaction and CoA modulation [ bioRxiv, 2024, 2024.02.22.581432]	PubMed: 38464226
A ribosomal gene panel predicting a novel synthetic lethality in non-BRCAness tumors [ Signal Transduct Target Ther, 2023, 8(1):183]	PubMed: 37160887
Genetic screens reveal new targetable vulnerabilities in BAP1-deficient mesothelioma [ Cell Rep Med, 2023, S2666-3791(22)00494-3]	PubMed: 36657447

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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