LDE225

2 mg

Cat. No.: 43-X52

$139.00

LDE225 (NPV-LDE225) is a novel and specific small molecule Smoothened (Smo) inhibitor with an IC₅₀ of 11nM. LDE225 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 nmol/l and almost complete regression at 1.5 μmol/l. 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 and partial inhibition was obtained when applying a 0.3% solution.

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TECHNICAL INFORMATION

Other Names: BCP000600/NVP-LDE225/LDE225

Chemical Formula:  C26H26F3N3O3

CAS Number: 956697-53-3

Molecular Weight: 485.5

Purity:  >99%

Appearance:  white solid 

Solubility: DMSO

 

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light. Following reconstitution, store  aliquots at -20°C. 

Stability: Stock solutions stable at -20°C for up to 2 years.

Shipping Conditions: Shipped at room temperature.

 

PRODUCT USE

Soluble in DMSO. If precipitate is observed,  vortex for 5 minutes.

 

References

Buonamici et al. (2010) Interfering with resistance to smoothened antagonists by inhibition of the PI3K pathway in medulloblastoma. Sci Transl Med. 2(51):51ra70.

Skvara et al. (2011) Topical treatment of Basal cell carcinomas in nevoid Basal cell carcinoma syndrome with a smoothened inhibitor. J Invest Dermatol. 131(8):1735-44.

Metcalfe et al. (2011) Hedgehog fights back: mechanisms of acquired resistance against Smoothened antagonists. Cancer Res. 71(15):5057-61.

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