Costunolide (NSC 106404), a natural sesquiterpene compound with multiple biological activities; inhibits FPTase with IC50 of 20 μM, also inhibits telomerase with IC50 of 65-90 μM.
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Costunolide Costunolide (NSC 106404), a natural sesquiterpene compound with multiple biological activities; inhibits FPTase with IC50 of 20 μM, also inhibits telomerase with IC50 of 65-90 μM. In vitro
Costunolide inhibits the growth and telomerase activity of MCF-7 and MDA-MB-231 cells in a concentration- and time-dependent manner. Costunolide also inhibits the farnesylation process of human lamin-B by farnesyl–proteinttransferase (FPTase), in a dose dependent manner. Continuously treatment of Costunolide for 48 hours will significantly decrease proliferation of human tumor cells (A549, SK-OV-3, SK-MEL-2, XF498 and HCT-1) in a dose-dependent manner. Costunolide induces apoptosis by ROS-mediated mitochondrial permeability transition and cytochrome C release to the cytosol in HL-60 human leukemia cells. A recent study indicates that Costunolide shows significant antifungal activity, including Trichophyton mentagrophytes, T.simlii, T.rubrum, and so on.
In vivo
Costunolide inhibits angiogenic response by blocking the angiogenic factor signaling pathway. In a mouse corneal micropocket assay, Costunolide reduces VEGF-stimulated neovascularization in mice. Cell Data
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