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

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Ro 48-8071 Chemical Structure

Ro 48-8071 Chemical Structure

CAS No. : 161582-11-2

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Ro 48-8071 Related Antibodies

Top Publications Citing Use of Products

    Ro 48-8071 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.

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    Description

    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]
    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: 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]
    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.

    Ro 48-8071 Related Antibodies
    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.
    Molecular Weight

    448.37

    Formula

    C23H27BrFNO2
    CAS No.
    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Ro 48-8071 Related Classifications

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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Ro 48-8071161582-11-2OthersInhibitorinhibitorinhibit

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