Cyclopamine inhibits activation of the Hedgehog response pathway by binding to and inhibiting the proto-oncogene Smoothened (SMO). The effects of oncogenic mutations that either activate SMO or inactivate the tumor suppressor Patched (Ptch) can be reversed by cyclopamine treatment. Cyclopamine has also been shown to induce apoptosis in colorectal adenoma cell lines, carcinoma-derived cell lines, and skin basal cell carcinomas and is being investigated as an anti-cancer drug.

≥99% by HPLC

Cyclopamine inhibits the activity for Hedgehog signaling-dependent motor neuron differentiation with IC50 = 300 nmol/L.

Soluble in ethanol, methanol and DMSO. Ethanol is the best solvent for biological use. To make a 2% solution, heat cyclopamine in ethanol to 50-60°C. In methanol or DMSO, solubility is 7 mg/ml and 4 mg/ml respectively.

White to off-white crystalline solid

Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

1. Taipale, J., et al., Nature 2000; 406: 944 – 945.
2. Chen, J.K., et al., Genes & Dev. 2002; 16: 2743 – 2748.
3. Qualtrough, D., et al., Int J Cancer. 2004; 110: 831-837.

Hedgehog Pathway

Inhibitor