Parthenolide

貨號 Cat. No.
P-250
規格 Size
10x1mg 5mg 5x5mg

Description

Parthenolide


Nuclear Factor-kB (NF-kB) Pathway Inhibitor











Product#: P-250

























Sizes:
10 x 1 mg
5 mg
5 x 5 mg
 
 
 














M.W.: 248.3










CAS No.: [20554-84-1]












Structure:
 








 










Purity: >99%












Bioassay:

Parthenolide inhibits NFkB pathway in Jurkat and HeLa cell lines. Jurkat (A) and HeLa (B) cells were preincubated with different concentrations of Parthenolide  (#P-250) as indicated in the figure for 60 min. Jurkat cells were stimulated with 100nM PMA (#P-800) and 1mM Ionomycin (#I-700) for 15 min and HeLa cells were stimulated with 4000U/ml TNFa  for 10 min. Cell lysates were subjected to Western blot analysis using a phospho-p65NFkB.


 












 







 









References:














































1.



Johnson, E. S. et al. (1985) Br. Med. J. 291, 569.



2.


Biggs, M. J. et al. (1982) Lancet 2, 776.

3.


Hall, I. H. et al. (1979) J. Pharmacol. Sci. 68, 537.

4.


Douros, J. and Suffness, M. (1978) Cancer Chemother. Pharmacol. 1, 91.

5.


Lee, K. H. et al. (1977) Science 196, 533.

6.


Bork, P. M. et al. (1997) FEBS Lett. 402, 85.

7.


Hehner, S. P. et al. (1999) J. Immunol. 163, 5617.

8.


Patel, N.M. et al. (2000) Oncogene 19, 4159.

9.


Wang, W. et al. (1999) Clin. Cancer Res. 5, 119.

10.



Wen, J. et al. (2002) J. Biol. Chem. 277, 38954.




Parthenolide is a sesquiterpene lactone found in Mexican-Indian medicinal plants such as Tanacetum parthenium. It has been widely used in indigenous medical practices for the treatment of migraine, inflammation and tumors.1-4 Parthenolide inhibits IkB kinase (IKK) and IKKb (the upstream activators of the Nuclear Factor-kB (NF-kB) pathway), thus inhibiting Interleukin 1- and tumor necrosis factor a (TNF a) without affecting the activation of p38 and c-Jun N-terminal kinase.5,6

In breast adenocarcinoma and pancreatic tumor cell lines which constitutively express active NF-kB, parthenolide inhibits NF-kB DNA binding and increases sensitivity to chemotherapeutic agents. The sensitivity of these tumor cells to parthenolide is due to the low expression level of the multifunctional detoxification enzyme glutathione S-transferase p caused by inhibition of NF-kB activity.7,10


 


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