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Biological Activity: Cyclopamine inhibits the activity for Hedgehog signaling-dependent motor neuron differentiation with IC50 = 300 nmol/L.
CAS Number: 4449-51-8
Description: 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.
Format: White to off-white crystalline solid
Purity: ≥99% by HPLC
Solubility: 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.
Storage Stability: 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.
Biosafety Level: Not applicable (BSL-1)
References: 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.