Cyclopamine

Catalog No.S1146

Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.

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Cyclopamine Chemical Structure

Cyclopamine Chemical Structure
Molecular Weight: 411.62

Validation & Quality Control

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Quality Control & MSDS

Related Compound Libraries

Hedgehog/Smoothened Inhibitors with Unique Features

  • Selective Smoothened inhibitor

    PF-5274857 Smoothened-selective, IC50=5.8 nM.

  • Smoothened Inhibitor in Clinical Trial

    LDE225 (NVP-LDE225,Erismodegib) Phase III for Hh-pathway activated relapsed Medulloblastoma (MB).

  • Newest Smoothened Inhibitor

    GANT61 Inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.

  • Smoothened Activator

    Purmorphamine Directly binds and activates Smoothened, and blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM.

Product Information

  • Compare Hedgehog/Smoothened Inhibitors
    Compare Hedgehog/Smoothened Products
  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.
Targets Smoothened [1]
(TM3Hh12 cells)
IC50 46 nM
In vitro Cyclopamine inhibits the Hedgehog signaling pathway with an IC50 of 46 nM, and blocks the activity of human Smo receptor expressed in CHO-K1 cells in [3H]Hh-Ag binding assay with an IC50 of 280 nM. [1] Cyclopamine significantly inhibits Hedgehog pathway activity in a dose-dependent manner in gut-derived tumor cell lines expressing Patched (PTCH) mRNA, and induces growth inhibition of those tumor cell lines by 75-95% at the concentration of 3 μM, but ineffective towards the colon tumor cells without PTCH mRNA expression, suggesting the effects of Cyclopamine treatment are Hedgehog pathway related rather than generally cytotoxic. [2] By blocking Hedgehog signaling through direct interaction with Smo, Cyclopamine (10 μM) inhibits the proliferation of SMOhigh Cyclopamine-responsive cell lines L3.6sl and Panc 05.04 by 75-80%, and increases the apoptosis by 2.5- to 3.5-fold, without affecting the BxPC3-SMOlow cell line. [3] Cyclopamine treatment significantly decreases of Snail mRNA and increasea E-cadherin transcripts in the E3LZ10.7 cell line. Independent of inhibition of cell growth, Cyclopamine treatment significantly inhibits the invasive phenotype of Hedgehog-dependent L3.6pl cells, causing a >500-fold reduction in the number of transmigrating cells, but not that of the Hedgehog-independent cell line Panc-1. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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... Click to View More Cell Line Experimental Data

In vivo Administration of Cyclopamine at dose of 50 mg/kg/day for 22 days eradicates the HUCCT1 xenografts in mice with no obvious adverse effects. [2] Cyclopamine treatment at dose of 1.2 mg for 7 days induces significant apoptosis of tumor cells and decreases the tumor mass by 50-60% in Panc 05.04- and L3.6sl-derived tumors, respectively, but not in the BxPC3-SMOlow tumors. [3] Administration of Cyclopamine alone profoundly inhibits tumor metastases in xenografts of E3LZ10.7 and L3.6pl, and completely abrogates metastases when in combination of gemcitabine. [4]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Hedgehog cell assay This assay measures the end stage of the Hh signaling pathway, that is, the transcriptional modulation of Gli, using Luciferase as readout (Gli-Luc assay). Cyclopamine is prepared for assay by serial dilution in DMSO and then added to empty assay plates. TM3Hh12 cells (TM3 cells containing Hh-responsive reporter gene construct pTA-8xGli-Luc) are resuspended in F12 Ham's/DMEM (1:1) containing 5% FBS and 15 mM Hepes pH 7.3, added to assay plates and incubated with Cyclopamine for approximately 30 minutes at 37 °C in 5% CO2. 1 nM Hh-Ag 1.5 is then added to assay plates and incubated at 37 °C in the presence of 5% CO2. After 48 hours, either Bright-Glo or MTS reagent is added to the assay plates and luminescence or absorbance at 492 nm is determined. IC50 value, defined as the inflection point of the logistic curve, is determined by non-linear regression of the Gli-driven luciferase luminescence or absorbance signal from MTS assay vs log10 (concentration) of Cyclopamine using the R statistical software pack

Cell Assay: [2]

Cell lines SEG1, OE33, KYAE, KYSE180, SNU1, AGS, SNU16, NCI-N-87, HUCCT1, PANC1, PL5, PL6, BXPC3, HS766T, KYSE150, GBD1, DLD1, and HCT116
Concentrations Dissolved in DMSO, final concentration 3 μM
Incubation Time 4 days
Method Cells are exposed to Cyclopamine in 96-well plates. Cell viability is measured by MTS (soluble tetrazolium salt) assay. 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).

Animal Study: [2]

Animal Models Athymic (nude) mice inoculated subcutaneously with HUCCT1 cells
Formulation Dissolved in DMSO, and diluted in saline
Dosages 50 mg/kg/day
Administration Subcutaneous injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Peukert S, et al. Bioorg Med Chem Lett, 2009, 19(2), 328-331.

[2] Berman DM, et al. Nature, 2003, 425(6960), 846-851.

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Chemical Information

Download Cyclopamine SDF
Molecular Weight (MW) 411.62
Formula

C27H41NO2

CAS No. 4449-51-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms 11-deoxojervine
Solubility (25°C) * In vitro DMF 10 mg/mL warming (24.29 mM)
Ethanol 2 mg/mL warming (4.85 mM)
Water <1 mg/mL (<1 mM)
In vivo 10% DMSO+30% PEG 300+5% Tween 80+ddH2O 1mg/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.
Chemical Name Spiro[9H-benzo[a]fluorene-9,2'(3'H)-furo[3,2-b]pyridin]-3-ol, 1,2,3,3'a,4,4',5',6,6',6a,6b,7,7',7'a,8,11,11a,11b-octadecahydro-3',6',10,11b-tetramethyl-, (2'R,3S,3'R,3'aS,6'S,6aS,6bS,7'aR,11aS,11bR)-

Customer Product Validation(4)


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Rating
Source Cancer Lett 2012 322, 169-176. Cyclopamine purchased from Selleck
Method Western blotting, real-time RT-PCR
Cell Lines pancreatic cancer cell
Concentrations 10 μM
Incubation Time 48 h
Results Cyclopamine significantly decreased pancreatic cancer invasion (Fig. A), reversed the down-regulation of E-cadherin and up-regulation of vimentin (Fig. B and C), and reduced the expression of Gli-1 even in the presence of SDF-1 (Fig. B).

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Rating
Source Cancer Res 2012 72, 2262-74. Cyclopamine purchased from Selleck
Method [3H]thymidine incorporation assay, Western blot
Cell Lines melanoma cells, A-375 cells
Concentrations 5-10 μmol/L
Incubation Time 48 h
Results Our results show that low concentrations of cyclopamine (5-10 μmol/L) were effective in blocking the proproliferative effects of Cav1KO-CM on B16F10 melanoma cells. Interestingly, the proliferation of B16F10 cells incubated with WT-CM containing cyclopamine remains unchanged (Fig. A). Similarly, cyclopamine prevented the proproliferative effects of conditioned medium from serum-activated hTBJ1-shCAV1 cells on A-375 human melanoma cells (Fig. B)

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Source Exp Hematol 2012 40, 418-27. Cyclopamine purchased from Selleck
Method MTT assay
Cell Lines CD34+ cells, CD34- cells
Concentrations 10 μM
Incubation Time 24/72 h
Results 10 μM cyclopamine was administered to CD34+ and CD34- cells. After 72 hours cultivation, total cell number was about 0.73-fold of control in CD34+ cells group (p < 0.001), and it was about 0.92-fold of control (p = 0.038) in CD34- cells group (Fig. A). Cyclopamine induced apoptosis of CD34+ progenitor cells and CD34- leukemia cells; however, CD34+ cells were more sensitive to cyclopamine than CD34- cells (p < 0.001). Cyclopamine also induced apoptosis of K562 cells in a time-dependent manner, as measured by MTT assay. This effect could not be salvaged by exogenous Shh peptide, confirming the fact that SMO locates downstream of SHH in Shh signaling (Fig. B)

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Rating
Source Dr. Yong-Weon Yi from Georgetown University Medical Center. Cyclopamine purchased from Selleck
Method MTT assays
Cell Lines UWB1.289 cells
Concentrations 0.01-100 μM
Incubation Time 72 h
Results Cyclopamine potently inhibited the survival of UWB1.289 cells.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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