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 p2Ptch-/-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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
SmoA1
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Quality Level: 100. Assay: ≥. 70% (sum of two isomers, HPLC). form: liquid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light. shipped in: dry ice. storage temp.: −. 70°C. Storage Class Code: 10 - Combustible liquids. WGK: WGK 1. Flash Point(F): 188.6 °F - (refers to pure substance). Flash Point(C): 87 °C - (refers to pure substance).- UPC:
- 51284022
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 239807-50UG