Cyclopamine is an antagonist of the Hedgehog (Hh) pathway, demonstrating an IC50 of 46 nM in cell assays focused on the Hh pathway. Additionally, it selectively targets and inhibits Smo[1].
体内研究
Cyclopamine treatment results in the sustained regression of xenograft tumors, with complete regression observed within 12 days in treated animals[2].
Administration of Cyclopamine (1.2 mg) inhibits the development of tumors from human pancreatic adenocarcinoma cells transplanted into nude mice[3].
体外研究
Utilizing small molecule inhibitors of the Hh pathway, such as HhAntag and Cyclopamine, which both interact with Smo, has been shown to lead to tumor remission in a genetic mouse model for medulloblastoma[1].
Functioning as a Hedgehog (Hh) pathway antagonist, Cyclopamine impedes cell proliferation. Its inhibitory effect on the Hh pathway activity and the growth of digestive tract tumor cell lines, at a concentration of 3 μM, is linked to the level of PTCHmRNA expression[2].
As a steroidal alkaloid, Cyclopamine disrupts Hh signaling by directly binding to Smo[3].
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