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GPCR/G Protein Hedgehog/Smoothened Cyclopamine

Cyclopamine

Catalog No. T2825   CAS 4449-51-8
Synonyms: 11-Deoxojervine

Cyclopamine, a Smoothened (Smo) antagonist (IC50: 46 nM in TM3Hh12 cells), belongs to the group of steroidal jerveratrum alkaloids.

Cyclopamine, CAS 4449-51-8
Pack Size Availability Price/USD Quantity
5 mg In stock 60.00
10 mg In stock 72.00
25 mg In stock 95.00
50 mg In stock 144.00
100 mg In stock 224.00
200 mg Inquiry 314.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Cyclopamine, a Smoothened (Smo) antagonist (IC50: 46 nM in TM3Hh12 cells), belongs to the group of steroidal jerveratrum alkaloids.
Targets&IC50 Smoothened : ic50 46 nM (TM3Hh12 cells),  
Kinase 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 [1].
Cell Research
Cells were cultured in triplicate in 96-well plates in assay media to which 5E1 monoclonal antibody, ShhNp and/or cyclopamine were added at 0 h at concentrations indicated in the main text. Viable cell mass was determined by optical density measurements at 490 nm (OD490) at 2 and 4 days using the CellTiter96 colorimetric assay. Relative growth was calculated as OD (day 4) 2 OD (day 2)/OD (day 2) [3].
Cell lines: SEG1, OE33, KYAE, KYSE180, SNU1, AGS, SNU16, NCI-N-87, HUCCT1, PANC1, PL5, PL6, BXPC3, HS766T, KYSE150, GBD1, DLD1, and HCT116
Animal Research
A total of 0.1 ml Hanks’ balanced salt solution and matrigel (1:1) containing 2 × 10^6 cells were injected subcutaneously into CD-1 nude mice. Tumours were grown for 4 days to a minimum volume of 125 mm3; treatment was initiated simultaneously for all subjects. Mice were 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 were excised from mice, weighed and then fixed for 3 h at 4 °C with 4% paraformaldehyde, embedded in paraffin wax and sectioned (6 ?m). Apoptotic cells were identified by TUNEL using recombinant Tdt as previously described29. Sections were 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 were chosen at random [5].
Animal Model: Athymic (nude) mice inoculated subcutaneously with HUCCT1 cells
Synonyms 11-Deoxojervine
Purity 98.31%
Molecular Weight 411.63
Formula C27H41NO2
CAS No. 4449-51-8

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 10mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
6. Ma W, et al. Reduced Smoothened level rescued Aβ-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. J Genet Genomics. 2018 May 20;45(5):237-246. 7. Zheng H T, Fu T, Zhang H Y, et al. Progesterone-regulated Hsd11b2 as a barrier to balance mouse uterine corticosterone[J]. Journal of Endocrinology. 2020, 244(1): 177-187.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Natural Compound Library for HTS Anti-cancer Compound Library Stem cell Differentiation Compound Library Neuronal Signaling Compound Library Human Endogenous Metabolite Compound Library GPCR Compound Library Wnt&Hedgehog&Notch Compound Library

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