General description
A cell-permeable steroidal lactone that displays antitumor, anti-inflammatory, radiosensitizing, and immunosuppressive properties. Potently inhibits angiogenesis both in vitro (IC50 = 12 nM against HUVEC proliferation) and in vivo (80% inhibition at 7 µg/kg/day in C57BL/6J mice, s.c.) and NF-κB activation (IC50 = 500 nM in TNF-α-induced endothelial cells) by targeting the ubiquitin-mediated proteasome pathway. At higher concentrations (~5 µM) also affects AP-1 transcription and induces cell death.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
A steroidal lactone that displays antitumor, anti-inflammatory, radiosensitizing, and immunosuppressive properties.
Product does not compete with ATP.
Reversible: no
Target IC50: 12 nM against angiogenesis in vitro by inhibiting HUVEC proliferation
Packaging
Packaged under inert gas
Warning
Toxicity: Carcinogenic / Teratogenic (D)
Other Notes
Mohan, R., et al. 2004. Angiogenesis7, 115.
Jeyaprakasam, B., et al. 2003. Life Sci.74, 125.
Devi, P.U., et al. 1995. Cancer Lett.95, 189.
Kupchan, S.M., et al. 1969. J. Org. Chem.34, 3858.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51112016
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 681535-1MG