1. Stem Cell/Wnt
    Metabolic Enzyme/Protease
  2. Hedgehog
    Smo
    Endogenous Metabolite
  3. Cyclopamine

Cyclopamine (Synonyms: 11-Deoxojervine)

Cat. No.: HY-17024 Purity: 99.97%
Handling Instructions

Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.

For research use only. We do not sell to patients.

Cyclopamine Chemical Structure

Cyclopamine Chemical Structure

CAS No. : 4449-51-8

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Customer Review

Based on 17 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Cyclopamine purchased from MCE. Usage Cited in: Int J Nanomedicine. 2017 Apr 20;12:3267-3280.

    The Smo inhibitor Cyclopamine suppresses the activity of Hedgehog–Gli1 signaling. The gene expression and protein production of Smo in MG63 osteoblasts after 7 days of incubation on the different titanium surfaces.

    Cyclopamine purchased from MCE. Usage Cited in: Neurochem Res. 2016 Apr;41(4):687-95.

    Western blot and RT-qPCR assays of BDNF protein and gene expressions in primary cortical neurons in different experimental conditions. Immunoblotting bands of BDNF protein.

    Cyclopamine purchased from MCE. Usage Cited in: Life Sci. 2017 Dec 15;191:82-89.

    ORS cells are exposed to 3% oxygen for 48 h in presence or absence of Shh pathway inhibitor cyclopamine (5 μM) or GANT61 (10 μM). Immunofluorescence assay using anti-PCNA antibody is performed to detect the proliferative ORS cells (red). Cell nuclei are counterstained with DAPI (blue).

    Cyclopamine purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jun 26;9:674.

    Cyclopamine and GANT61 decrease the level of Gli1 as evidenced by western blot.

    Cyclopamine purchased from MCE. Usage Cited in: Cell Death Dis. 2019 Sep 12;10(9):681.

    Endometrial stromal cells are stimulated with 10 ng/mL TGFβ1 for 48 h. Then these cells are treated with 10 μM Cyc for 24 h and/or cocultured with 10 ng/mL VEGF165 for another 12 or 24 h. The protein levels of collagen 1, α-SMA and smad7 are examined.

    Cyclopamine purchased from MCE. Usage Cited in: Cell Death Dis. 2019 Sep 12;10(9):681.

    Endometrial stromal cells are stimulated with 10 ng/mL TGFβ1 for 48 h. Then these cells are treated with 10 μM Cyc for 24 h and/or cocultured with 10 ng/mL VEGF165 for another 12 or 24 h. The protein levels of collagen 1, α-SMA and smad7 are examined.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.

    IC50 & Target

    Human Endogenous Metabolite

     

    In Vitro

    Treatment with small molecule Hh inhibitors such as HhAntag and the natural product Cyclopamine, both binding to Smo, induces tumor remission in a genetic mouse model of medulloblastoma[1]. Cyclopamine is a Hedgehog (Hh) pathway antagonist. Cyclopamine suppresses cell growth. Cyclopamine (3 μM) suppression of Hh pathway activity and growth in digestive tract tumour cell lines correlates with expression of PTCHmRNA[2]. Cyclopamine is a steroidal alkaloid that inhibits Hh signalling through direct interaction with Smo[3].

    In Vivo

    Cyclopamine causes durable regression of xenograft tumors. Tumors in Cyclopamine-treated animals, regress completely by 12 days[2]. Cyclopamine (1.2 mg) treatment blocks tumour formation of human pancreatic adenocarcinoma cells after transplantation into nude mice[3].

    Molecular Weight

    411.62

    Formula

    C₂₇H₄₁NO₂

    CAS No.

    4449-51-8

    SMILES
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    Ethanol : 16.67 mg/mL (40.50 mM; Need ultrasonic)

    DMSO : 5 mg/mL (12.15 mM; Need ultrasonic and warming)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4294 mL 12.1471 mL 24.2943 mL
    5 mM 0.4859 mL 2.4294 mL 4.8589 mL
    10 mM 0.2429 mL 1.2147 mL 2.4294 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 0.5 mg/mL (1.21 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 0.5 mg/mL (1.21 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 0.5 mg/mL (1.21 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% EtOH    90% corn oil

      Solubility: ≥ 1.67 mg/mL (4.06 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [2]

    Cells are cultured in triplicate in 96-well plates in assay media to which 5E1 monoclonal antibody, ShhNp and/or Cyclopamine (3 μM) are added at 0 h at concentrations indicated in the main text. Viable cell mass is determined by optical density measurements at 490 nm (OD490) at 2 and 4 days using the CellTiter96 colorimetric assay. Relative growth is calculated as OD (day 4)-OD (day 2)/OD (day 2)[2].

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

    Animal Administration
    [3]

    Mice[3]
    A total of 0.1 mL Hanks’ balanced salt solution and matrigel (1:1) containing 2×106 cells is injected subcutaneously into CD-1 nude mice. Tumors are grown for 4 days to a minimum volume of 125 mm3; treatment is initiated simultaneously for all subjects. Mice are injected subcutaneously with vector alone (triolein:ethanol 4:1 v/v) or a Cyclopamine suspension (1.2 mg per mouse in triolein:ethanol 4:1 v/v) daily for 7 days. At the end of the treatment period, tumours are excised from mice, weighed and then fixed for 3 h at 4°C with 4% paraformaldehyde, embedded in paraffin wax and sectioned (6 µm). Apoptotic cells are identified by TUNEL using recombinant Tdt. Sections are then counterstained with eosin. Eight ×20-magnified fields from regions corresponding to the exterior, middle and interior of two control and two cyclopamine-treated tumours are chosen at random. We counted the number of TUNEL-positive nuclei manually. Haematoxylin/eosin staining is done.

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

    References

    Purity: 99.97%

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    Keywords:

    Cyclopamine11-DeoxojervineHedgehogSmoEndogenous MetaboliteSmoothenedInhibitorinhibitorinhibit

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    Product Name:
    Cyclopamine
    Cat. No.:
    HY-17024
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