Biochem/physiol Actions

Primary TargetSmoA1

Cell permeable: yes

General description

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. The solid form of this compound (Cat. No. 239804) is also available.

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

Packaged under inert gas

50 µg in Glass bottle

Physical form

A 1 mM (50 µg/72 µL) solution of Cyclopamine-KAAD (Cat. No. 239804) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.

Warning

Toxicity: Irritant (B)