LY 294002

貨號 Cat. No.
L-300
規格 Size
10 x 0.25 mg 1 mg 5mg 5x5mg

Description

LY 294002



A Specific Inhibitor of PI 3-Kinase












Product#: L-300

























Sizes:
10 x 0.25 mg
1 mg
5 mg
5 x 5 mg
 
 














M.W.: 307.35










CAS No.:

[154447-36-6]














Structure:
.








 










Purity: >99%












Bioassay:
The biological activity was tested to confirm the ability of LY 294002 to inhibit PI 3 - Kinase.

 













 


NIH/3T3 cells were preincubated for 30 min in different concentrations of LY294002 or Wortmannin,

and then stimulated with PDGF (3ng/ml) for 20 min. The cell extracts were blotted and probed

with (A) Phosphorylated- AKT antibody, followed by stripping and re-probing with (B) antibody to Akt protein.









 









References:










































1.



Kapeller, R. et al. (1994) Bioessays 16, 565.



2.


Duronio, V. et al. (1998) Cell Signal. 10, 233.

3.


Vlahos, C.J. et al. (1994) J. Biol. Chem. 269, 5241.

4.


Vlahos, C.J. et al. (1995) J. Immunol. 154, 2413.

5.


Curnock, A.P. et al. (1998) Cell. Immunol. 187, 77.

6.


Nicholson, K.M. et al. (2003) Cancer Lett. 190, 31.

7.


Coffer, P.J. et al. (1998) Biochem. J. 335 ( Pt 1), 1.

8.


Shao, J. et al. (2004) Cancer Res. 64, 229.

9.



Vivanco, I. et al. (2002) Nat. Rev. Cancer 2, 489.




PI 3-kinase is an enzyme implicated in growth factor signal transduction by associating with receptor and non-receptor tyrosine kinases. 1, 2 LY-294002 is a potent and specific cell-permeable inhibitor of Pl 3-kinase that acts on the ATP-binding site of the enzyme.3

In in vitro assays it displays an IC50 of 1.4 ç„¶ on purified PI 3-kinase, but did not inhibit PKC, PKA, MAP kinase and PI 4-kinase.3 In fMet-Leu-Phe stimulated neutrophils, LY-294002 completely abolished PI 3-kinase activity at 50 ç„¶.4 LY-294002 induces apoptosis in many cell types by blocking the PI3-K/Akt anti-apoptotic pathway.5, 6 Thus LY-294002 is useful tool for identifying the biochemical events regulated by the PI3-K/Akt pathway.7 This pathway has important relevance to the cellular events involved in cancer.6, 8, 9


 


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