Chemical Name
Spiro[9H-benzo[a]fluorene-9,2(3H)-furo[3,2-b]pyridin]-3-ol, 1,2,3,3a,4,4,5,6,6,6a,6b,7,7,7a,8,11,11a,11b-octadecahydro-3,6,10,11b-tetramethyl-, (2R,3S,3R,3aS,6S,6aS,6bS,7aR,11aS,11bR)-
In vitro
Cyclopamine can inhibit Hedgehog (Hh) signaling pathway by inhibiting Smoothened (Smo) with IC50 of 46 nM. Cyclopamine inhibits Hedgehog signaling by directly binding to the heptahelical bundle of Smoothened (Smo). Besides binding to Smo, cyclopamine also can reverse the retention of partially misfolded Smo in the endoplasmic reticulum, presumably through binding-mediated effects on protein conformation.
In vivo
At low concentrations, combination of cyclopamine and gefitinib can inhibit the growth of EGF plus SHH-stimulated and serum-stimulated androgen-responsive LNCaP-C33 and androgen-independent LNCaP-C81, DU145, and PC3 cells. combination of cyclopamine and gefitinib also can cause a higher rate of apoptotic death of prostate cancer cells compared with individual agents.
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