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Cat. No. Name Size Price Add Cart
KI0148Cyclopamine5 mg$100
Cyclopamine10 mg$170
Cyclopamine25 mg$350
Cyclopamine50 mg$640

Chemical Characteristic

Product NameCyclopamine
CAS No.4449-51-8
Molecular Weight 411.62
FormulaC27H41NO2
Chemical NameSpiro[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)-
SmilesC1[C@@H]2[C@@]3(C(=CC[C@H]2[C@@H]2CC[C@@]4(C(=C12)C)O[C@H]1[C@@H](NC[C@H](C1)C)[C@H]4C)C[C@H](CC3)O)C
Chemical Structure

Biological activities

Cyclopamine is a specific and potent Hedgehog (Hh) signal transduction pathway antagonist of Smoothened (Smo) with an IC50 of 46 nM.[1] In a panel of 21 human pancreatic cancer cell lines (including Capan-1, MIAPaCa, PL-3, XPA-4 and PL-11), cyclopamine (6 µM) reduces viable cell masses by nearly 100% to 0% as compared with solvent-treated cells. Cyclopamine induces a >500-fold reduction in the number of transmigrating Hh-dependent L3.6pl cells.[2] Cyclopamine (3 µM) significantly inhibits Hedgehog pathway activity in a dose-dependent manner in tumor cell lines from the oesophagus, stomach, biliary tract and pancreas expressing Patched (PTCH) mRNA, and induces growth inhibition by 75-95%.[3] In U87-MG cells, cyclopamine (5 and 10 µM) reduces Hh pathway activity in a dose-dependent fashion. Cyclopamine also inhibits endogenous Gli1 mRNA expression in U87-MG cells by 21% at 5 µM and 51% at 10 µM levels. In the high-Gli U87-MG and A172 lines, cyclopamine (10 µM) essentially abolishes the cell growth, whereas the increase in cell mass in the low-Gli CJ-MG and BK-MG lines is unaffected by cyclopamine. Colony formation is inhibited in a dose-dependent manner, with a significant 46% reduction in colonies grown in 5 µM cyclopamine and an approximately 90% reduction in colonies grown in 10 µM cyclopamine.[4]Zebrafish embryos treated with cyclopamine display defects in adult hematopoietic stem cell (HSC) formation. Cyclopamine targets Stem-Like Glioma Cells and blocks tumor engraftment. In an orthotopic xenograft model of pancreatic cancer, cyclopamine (25 mg/kg) profoundly inhibits metastatic spread. Only one of seven cyclopamine-treated mice develops pulmonary micrometastases versus seven of seven mice with multiple macrometastases in control animals. Combination of gemcitabine and cyclopamine completely abrogates metastases while also significantly reducing the size of primary tumors.[2] In HUCCT1 carcinoma cells xenografts model, cyclopamine (50 mg/kg/day) has a complete and durable tumoricidal effect of blocking the Hh pathway.[3]

Protocols

Cyclopamine is prepared for assay by serial dilution in DMSO and then added to empty assay plates. [1]

References

[1] Peukert S, et al. Identification and structure-activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway. Bioorg Med Chem Lett. 2009, 19(2): 328-331.
[2] Feldmann G, et al. Blockade of hedgehog signaling inhibits pancreatic cancer invasion and metastases: a new paradigm for combination therapy in solid cancers. Cancer Res. 2007, 67(5): 2187-2196.
[3] Berman DM, et al. Widespread requirement for Hedgehog ligand stimulation in growth of digestive tract tumours. Nature. 2003, 425(6960): 846-851.
[4] Bar EE, et al. Cyclopamine-mediated hedgehog pathway inhibition depletes stem-like cancer cells in glioblastoma. Stem Cells. 2007, 25(10): 2524-2533.

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