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Cyclopamine
(Synonyms11-deoxojervine
)
M.Wt: 411.62
Formula: C27H41NO2
Solubility: DMSO
Purity: >99%
Storage: at -20℃ 2 years
CAS No.: 4449-51-8
Price and Availability of Cyclopamine:
HedgehogBiological Activity of Cyclopamine:
Cyclopamine inhibits the hedgehog signaling pathway (Hh) by influencing the balance between the active and inactive forms of the Smoothened protein. The hedgehog signaling pathway carries out important functions in embryonic development when it goes awry, deformities can occur. However, errant activation of the pathway can also trigger cancer in adult humans[1] .
Cyclopamine is a lipophilic compound extracted from the lily Veratrum californicum. It antagonizes Smo activity by binding to its heptahelical bundle. Thus, it can block pathway activation resulting in any of the two upstream events of Smo—i.e., either from PTCH mutations or from Hh ligand over-expression. Cyclopamine is currently being investigated as a treatment agent in basal cell carcinoma, medulloblastoma, and rhabdomyosarcoma, tumors connected to excessive Hh activity, etc. [3]
In preclinical models of rodent and human prostate cancer, cyclopamine can inhibit tumor growth as well as tumor progression. Administration of cyclopamine causes both down-regulation of proliferation and initiation of apoptosis, with consequent reduction in tumor size. Administration of cyclopamine in a lethal, metastatic rodent model of prostate cancer completely abrogates systemic metastases and dramatically improves survival[2] .
References on Cyclopamine:
[1] Chen JK et al. Genes Dev. 2002 Nov 1;16(21):2743-8
[2] Kumar SK et al. Bioorg Med Chem. 2008 Mar 15;16(6):2764-8
[3] Bar EE et al. Stem Cells. 2007 Oct;25(10):2524-33
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