Art. -Nr.: HY-18630

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Ro 48-8071 free base

Name: Ro 48-8071 free base
Brand: MedChemExpress
SKU: HY-18630
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13 Cited Publications

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Based on 13 publication(s) in Google Scholar

Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC₅₀ of appr 6.5 nM.

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CAS. Nr.: 161582-11-2
Formel: C₂₃H₂₇BrFNO₂
Molecular Weight:448.37

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

Ro 48-8071 free base Chemical Structure

CAS. Nr.: 161582-11-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Protokoll
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC₅₀ of appr 6.5 nM.

IC₅₀ & Target

IC50: appr 6.5 nM (Oxidosqualene cyclase)^[1]

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Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	0.092 μM Compound: Ro 48-8071	Inhibition of total cholesterol biosynthesis in human HL60 cells assessed as incorporation of 2-13C-acetate by GC-MS analysis Inhibition of total cholesterol biosynthesis in human HL60 cells assessed as incorporation of 2-13C-acetate by GC-MS analysis	[PMID: 26745812]
HL-60	IC₅₀	8 μM Compound: Ro 48-8071	Cytotoxicity against human HL60 cells after 24 hrs by MTT assay Cytotoxicity against human HL60 cells after 24 hrs by MTT assay	[PMID: 23583910]
HL-60	IC₅₀	8 μM Compound: Ro 48-8071	Cytotoxicity against human HL60 cells after 24 hrs by MTT assay Cytotoxicity against human HL60 cells after 24 hrs by MTT assay	[PMID: 26745812]

In Vitro

In HepG2 cells, Ro 48-8071 reduces cholesterol synthesis dose dependently with an IC₅₀ value of appr 1.5 nM^[1]. Ro 48-8071 (10 μM) significantly reduces the viability of PC-3 prostate cancer cells, but not normal prostate cells. Ro 48-8071 (10-30 μM) induces apoptosis of both LNCaP and C4-2 cell lines in a dose-dependent manner. And castration-resistant PC-3 and DU145 cells also demonstrate significant levels of apoptosis following 24-hour treatment with Ro 48-8071. Ro 48-8071 (10-25 μM) reduces AR protein expression in a dose-dependent manner. Ro 48-8071 (0.1-1 μM) increases ERβ protein expression dose-dependently in both hormone-dependent LNCaP and castration-resistant PC-3 cells^[2]. Using mammalian cells engineered to express human ERα or ERβ protein, together with an ER-responsive luciferase promoter, Ro 48-8071 dose-dependently inhibits 17β-estradiol (E2)-induced ERα responsive luciferase activity (IC₅₀, appr 10 μM), under conditions that are non-toxic to the cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ro 48-8071 lowers LDL-C maximally appr 60% at 150 μmol/kg per day, with no further reduction up to 300 μmol/kg per day, leaving HDL-C unchanged at all doses in hamsters. Ro 48-8071 (≥00 μmol/kg per day) increases the amount of MOS in liver of hamsters. Ro 48-8071 (300 μmol/kg per day) remarkedly and significantly reduces VLDL secretion of hamsters^[1]. Ro 48-8071 (5 or 20 mg/kg) significantly reduces in vivo tumor growth in mice, without weight loss of the mice. Furthermore, Ro 48-8071 at a concentration of 20 mg/kg, completely eradicates two of the 12 tumors being monitored in the mice in the timeframe tested^[2]. Ro 48-8071 (20 mg/day/kg body weight) leads to a rapid and sustained inhibition (>50%) of cholesterol synthesis in the whole small intestine of BALB/c mice. Sterol synthesis is also reduced in the large intestine and stomach^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 161582-11-2
Molecular Weight 448.37
Formel C₂₃H₂₇BrFNO₂
SMILES

O=C(C1=CC=C(Br)C=C1)C2=CC=C(OCCCCCCN(C)CC=C)C=C2F
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (13)

All Cell Proliferation/Viability AssayFlow CytometryWBIn Vivo Efficacy StudyIF

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Journal Impact Factor

Cancer Cell

Exhaustion-associated cholesterol deficiency dampens the cytotoxic arm of antitumor immunity. [Abstract]

2023 Jul 10;41(7):1276-1293.e11. PMID: 37244259
Nat Commun

A polycistronic system for multiplexed and precalibrated expression of multigene pathways in fungi. [Abstract]

2023 Jul 17;14(1):4267. PMID: 37460548
Mol Cell

The ZMYND8-regulated mevalonate pathway endows YAP-high intestinal cancer with metabolic vulnerability. [Abstract]

2021 Jul 1;81(13):2736-2751.e8. PMID: 33932349
Cell Death Dis

Targeting epigenetic modulation of cholesterol synthesis as a therapeutic strategy for head and neck squamous cell carcinoma. [Abstract]

2021 May 13;12(5):482. PMID: 33986254
Cell Death Discov

Inhibition of lanosterol synthase linking with MAPK/JNK signaling pathway suppresses endometrial cancer. [Abstract]

2025 Feb 8;11(1):55. PMID: 39922821

Ro 48-8071 free base purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]

The results of CCK8 reflected the IC₅₀ of Ro 48-8071 (0-2 μM) in EC cells and that Ro 48-8071 significantly inhibited the proliferation of EC cells.

Ro 48-8071 free base purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]

Clone formation and Transwell experiments showed that the activity of EC cells was significantly inhibited by Ro 48-8071 (0-1 μM).

Ro 48-8071 free base purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]

Flow cytometry analysis found that Ro 48-8071 (0-1 μM) can promote the apoptosis of EC cells.

Ro 48-8071 free base purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]

Ro 48-8071 (0-1 μM) reduces the expression of phosphorylated JNK protein.

Ro 48-8071 free base purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]

Images of isolated tumors from the subcutaneous tumor nude mice model established using Ishikawa cells treated with Ro 48-8071 or SP600125(n = 6 mice per group).
Sci China Life Sci

NPC1-regulated dynamic of clathrin-coated pits is essential for viral entry. [Abstract]

2022 Feb;65(2):341-361. PMID: 34047913
Cell Rep

EGFR-phosphorylated GDH1 harmonizes with RSK2 to drive CREB activation and tumor metastasis in EGFR-activated lung cancer. [Abstract]

2022 Dec 13;41(11):111827. PMID: 36516759
Mol Med Rep

Cholesterol biosynthesis inhibitor RO 48‑8071 inhibits pancreatic ductal adenocarcinoma cell viability by deactivating the JNK and ERK/MAPK signaling pathway. [Abstract]

2021 Dec;24(6):828. PMID: 34590153
Neoplasia

Cholesterol biosynthesis as a drug-induced vulnerability in diffuse large B cell lymphoma insensitive to EZH2 inhibition. [Abstract]

2025 Oct 27:70:101243. PMID: 41151153
ACS Synth Biol

CMI: CRISPR/Cas9 Based Efficient Multiplexed Integration in Saccharomyces cerevisiae. [Abstract]

2023 May 19;12(5):1408-1414. PMID: 36853024
Cancer Res Commun

Synergistic effects of PARP inhibition and cholesterol biosynthesis pathway modulation. [Abstract]

2024 Sep 1;4(9):2427-2443. PMID: 39028932
Immunomedicine

Metabolic inhibitor screening identifies dihydrofolate reductase as an inducer of the tumor immune escape mediator CD24. [Abstract]

2022 Dec;2(2):e1041. PMID: 36816458
Oncotarget

Disabled cell density sensing leads to dysregulated cholesterol synthesis in glioblastoma. [Abstract]

2017 Feb 28;8(9):14860-14875. PMID: 28118603

Ro 48-8071 free base purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Feb 28;8(9):14860-14875. [Abstract]

Cell death in TS600 glioma cells. Dead cells are visualized with SYTOX Orange 24 hours after treatment with DMSO (mock), 1 μM epirubicin, 10 μM clotrimazole, 5 μM ketoconazole, or 1 μM Ro 48-8071.

Protokoll

Animal Administration^[2]

Six-week-old male athymic nude mice (nu/nu) weighing 20-22 g are used in the assay. Castration-resistant PC-3 cells (5×10⁶ in 0.15 mL solution) are mixed with matrigel and RPMI-1640 medium (1/1, v/v) and injected subcutaneously into both flanks of each mouse (n=6 animals/group) and tumors allowed to develop. The tumors are measured twice per week with a digital caliper. Tumor volumes are calculated by the formula (L × W × H) × π/6. Drug treatment is started when tumor volumes reach appr 100 mm³. Mice are given daily tail vein injections of 0.1 mL solution of either 5 or 20 mg/kg Ro 48-8071 for 5 days. This is followed by an injection every other day for six additional treatments and then a final injection 2 hours prior to sacrifice. Control mice receive the same volume of phosphate-buffered saline on the same schedule. The animals are weighed and tumor volumes are measured twice weekly throughout the drug treatment period.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Morand OH, et al. Ro 48-8.071, a new 2,3-oxidosqualene:lanosterol cyclase inhibitor lowering plasma cholesterol in hamsters, squirrel monkeys, and minipigs: comparison to simvastatin. J Lipid Res. 1997 Feb;38(2):373-90. [Content Brief]

[2]. Liang Y, et al. Cholesterol biosynthesis inhibitor RO 48-8071 suppresses growth of hormone-dependent and castration-resistant prostate cancer cells. Onco Targets Ther. 2016 May 30;9:3223-32 [Content Brief]

[3]. Liang Y, et al. Cholesterol biosynthesis inhibitors as potent novel anti-cancer agents: suppression of hormone-dependent breast cancer by the oxidosqualene cyclase inhibitor RO 48-8071. Breast Cancer Res Treat. 2014 Jul;146(1):51-62. [Content Brief]

[4]. Chuang JC, et al. Sustained and selective suppression of intestinal cholesterol synthesis by Ro 48-8071, an inhibitor of 2,3-oxidosqualene:lanosterol cyclase, in the BALB/c mouse. Biochem Pharmacol. 2014 Apr 1;88(3):351-63. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

Ro 48-8071 free base

13 Cited Publications

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Ro 48-8071 free base

Publications Citing Use of MedChemExpress (MCE) Ro 48-8071 free base

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen