High affinity and selective Smoothened (Smo) receptor antagonist (Ki
= 4.6 nM). Exhibits >1000-fold selectivity for Smo over a panel of other receptors, ion channels and enzymes. Inhibits Shh-induced Hedgehog signaling in MEF cells. Induces tumor regression in a medulloblastoma allograft mouse model. Orally available and brain penetrant.
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All Tocris products are intended for laboratory research use only.
Sold for research purposes under agreement from Pfizer Inc.
Effective targeting of Hedgehog signaling in a medulloblastoma model with PF-5274857, a potent and selective Smoothened antagonist that penetrates the blood-brain barrier.
Rohner et al.
Mol.Cancer Ther., 2011;11:57