LDE225 is a novel and specific, orally bioavailable Smo inhibitor with an IC50 of 11 nM. It has been shown to potentially inhibit Hh-and Smo-dependent proliferation in vivo. It also induced the regression of preformed basaloid lesions with an IC50 of <150 nM and almost complete regression at 1.5 μM. Topical application of a 1% LDE225 solution to depilated skin of C57/BL6 mice completely inhibited hair growth during anagen phase as well as the expression of the Hh-pathway target genes (Gli1, Gli2, Sox9, and N-Myc) and partial inhibition was obtained when applying a 0.3% solution.
Technical information:
Chemical Formula: | C26H26F3N3O3 | |
CAS #: | 956697-53-3 | |
Molecular Weight: | 485.50 | |
Purity: | >98% | |
Appearance: | White solid | |
Chemical Name: | N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-2-methyl-4'-(trifluoromethoxy)biphenyl-3-carboxamide | |
Solubility: | Up to 50 mM in DMSO |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
1. | Shifeng Pan et al. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med. Chem. Lett., 2010, 1 (3), pp 130–134. |
Other Information:
Product Specification (pdf)
MSDS (pdf)