Biochem/physiol Actions

Reversible: no

Target IC₅₀: 20 nM against Hedgehog (Hh) signaling in Shh-LIGHT2 assay; 50 nM in p2Ptch-/-cells; 500 nM in SmoA1-LIGHT cells

Product does not compete with ATP.

Primary TargetHh signaling in Shh-light2 assay

Cell permeable: yes

General description

A potent, cell-permeable analog of Cyclopamine (Cat. No. 239803) that specifically inhibits the Hedgehog (Hh) signaling with similar or lower toxicity (IC₅₀ = 20 nM in Shh-LIGHT2 assay; 50 nM in p2^Ptch-/-cells; 500 nM in SmoA1-LIGHT cells). Binds to SmoA1 and promotes its exit from the endoplasmic reticulum. Suppresses both the ShhNp-induced pathway activity and SmoA1-induced reporter activity. Shown to sensitize human glioma cells to TRAIL-induced apoptosis. Also available as a 1 mM solution in DMSO (Cat. No. 239807).

A cell-permeable potent analog of Cyclopamine (Cat. No. 239803) that specifically inhibits Hedgehog (Hh) signaling with similar or lower toxicity (IC₅₀ = 20 nM in Shh-LIGHT2 assay; 50 nM in p2^Ptch-/-cells; 500 nM in SmoA1-LIGHT cells). Binds to SmoA1 and promotes its exit from the endoplasmic reticulum. Suppresses both ShhNp-induced pathway activity and SmoA1-induced reporter activity. Reported to cause regression of murine tumor allografts in vivo and induce rapid cell death in human medulloblastoma. Shown to sensitize human glioma cells to TRAIL-induced apoptosis.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Siegelin, M.D. et al. 2009. Neurobiol. Dis.34, 259.Watkins, D.N., et al. 2003. Nature422, 313.Berman, D.M., et al. 2002. Science297, 1559.Chen, J.K., et al. 2002. Proc. Natl. Acad. Sci. USA99, 14071.Chen, J.K., et al. 2002. Genes Dev.16, 2743.Frank-Kamenetsky, M., et al. 2002. J. Biol.1, 10.Taipale, J., et al. 2000. Nature406, 1005.

Packaging

100, 500 µg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 weeks at -20°C.

Warning

Toxicity: Harmful (C)