Catalog No.S1319 Synonyms: NSC 106404
Molecular Weight(MW): 232.32
Costunolide, 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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Choose Selective Telomerase Inhibitors
|Description||Costunolide, a natural sesquiterpene compound with multiple biological activities; inhibits FPTase with IC50 of 20 μM, also inhibits telomerase with IC50 of 65-90 μM.|
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. |
Telomerase activity assay:The telomerase activity is measured by the TRAP assay using the TRAPez Telomerase Detection Kit, which includes primers of a 36-bp internal control (IC) for quantifying the amplification of telomerase activity within a linear range close to 2.5 logs. For RNase treatment, 10μL of extract are incubated with 1μg of RNase at 37 °C for 20 minutes. The products of the TRAP assay are resolved by electrophoresis in a nondenaturing12% PAGE in a buffer containing 0.5 × Tris–borate EDTA and detected by autoradiograph. For quantification of TRAP products, the dried gels are exposed to Fuji Imaging Plate at room temperature. Results are corrected for background, and a standard value of 100 is given to the untreated control cell signal. Signal intensities of Costunolide-treated cells are compared to the standard and are expressed as a fraction of the maximum value of 100. 
-  Choi SH, et al, Cancer Lett, 2005, 227(2), 153-162.
-  Park SH, et al, Planta Med, 2001, 67(4), 358-359.
-  Lee MG, et al, Biol Pharm Bull, 2001, 24(3), 303-306.
|In vitro||DMSO||47 mg/mL (202.3 mM)|
|Ethanol||1 mg/mL (4.3 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+corn oil
For best results, use promptly after mixing.
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