tcsc0633 Cyclopamine (11-Deoxojervine)

Cyclopamine is a Hedgehog (Hh) pathway antagonist with IC₅₀ of 46 nM in the Hh cell assay.

IC50 & Target: IC50: 46 nM (Hedgehog, in Hh cell assay)^[1]

In Vitro: Treatment with small molecule Hh inhibitors such as HhAntag and the natural product Cyclopamine, both binding to Smo, induces tumor remission in a genetic mouse model of medulloblastoma^[1]. Cyclopamine is a Hedgehog (Hh) pathway antagonist. Cyclopamine suppresses cell growth. Cyclopamine (3 μM) suppression of Hh pathway activity and growth in digestive tract tumour cell lines correlates with expression of PTCHmRNA^[2]. Cyclopamine is a steroidal alkaloid that inhibits Hh signalling through direct interaction with Smo^[3].

In Vivo: Cyclopamine causes durable regression of xenograft tumors. Tumors in Cyclopamine-treated animals, regress completely by 12 days^[2]. Cyclopamine (1.2 mg) treatment blocks tumour formation of human pancreatic adenocarcinoma cells after transplantation into nude mice^[3].