Catalog Number: 5262
Chemical Name: 1-[4-(5'-Chloro-3,5-dimethyl[2,4'-bipyridin]-2'-yl-1-piperazinyl]-3-(methylsulfonyl)-1-propanone hydrochloride
Biological Activity
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. 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
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