Biochem/physiol Actions

Reversible: no

Primary TargetA steroidal lactone that displays antitumor, anti-inflammatory, radiosensitizing, and immunosuppressive properties.

Product does not compete with ATP.

Cell permeable: yes

Target IC₅₀: 12 nM against angiogenesis in vitro by inhibiting HUVEC proliferation

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.

Legal Information

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

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.

Packaging

1, 5 mg in Plastic ampoule

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)