Genistein

貨號 Cat. No.
G-300
規格 Size
10 x 1 mg 10mg 5x10mg 25mg 5x25mg 100mg

Description


Genistein


A Tyrosine Kinase Inhibitor




 












Product#: G-300

























Sizes:
10 x 1 mg
10 mg
5 x 10 mg
25 mg
5 x 25 mg
100 mg














M.W.: 270.2 Daltons










CAS No.:

[446-72-0]














Structure:
.








 










Purity: >99%












Bioassay:
The biological activity was tested to confirm the ability of Genistein to inhibit tyrosine kinase activity in Hela cells.










Hela cells were grown to 70% confluence then the cells serum starved for 18 h. The cells were preincubated for 30 min in presence or absence of 500 nM Genistein and then simulated for 2 h with 20% fetal calf serum or culture medium. The cell extracts were blotted and probed with p-Tyr specific antibodies.







 









References:














































1.



Polkowski, K. and Mazurek, A.P. (2000) Acta Pol. Pharm. 57, 135. Review.



2.


Sarkar, F.H. and Li, Y. (2002) Cancer and Metastasis Reviews 21, 265. Review.

3.


Salti, G.I (2000) Eur. J. Cancer. 36, 796.

4.


Spinozzi, F. et al. (1994) Leuk. Res. 18, 431.

5.


Constantinou, A. et al. (2003) Cancer Sci. 94, 215.

6.


Li, Y. and Sarkar, F.H. (2002) Cancer Lett. 186, 157.

7.


Huang, R.Q. et al. (1999) Brain Res. Mol. Brain Res. 67, 177.

8.


Constantinou, A. and Huberman, E. (1995) Proc. Soc. Exp. Biol. Med. 208, 109. Review.

9.


Khoshyomn, S. et al. (2002) J. Neurooncol 57, 193.

10.



Tamura, S. et al. (2003) Pigment Cell Res. 16, 470.




An isoflavonoid derived from soy products.1 Genistein inhibits protein tyrosine kinases, including the EGF receptor kinase (IC50 = 2.6 uM). The inhibition is competitive with respect to ATP and non-competitive with respect to the phosphate acceptor.1,2 It has a trivial effect on the activity of PKA and PKC (IC50 > 350 uM).1,2 In addition, Genistein inhibits Topoisomerase II activity,3 cause cell cycle arrest and apoptosis in Jurkat T-leukemia cells.4 It down regulates the transcription of genes involved in angiogenesis,5,6 and inhibit the action of GABA on recombinant GABA-A receptors.7 Genistein also inhibits tumor cell proliferation and induces tumor cell differentiation. 8-10


 

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