LY 294002, 4′-NH2 is a cell permeable 4′-amino derivative which inhibits the p110α, p110β, p110δ, and p110γ subunits of PI 3-kinase. LY 294002, 4′-NH2 functions by preventing the phosphorylation of Akt1 in the PI 3-kinase/Akt1/mTOR pathway. In addition, the 4′ end of LY 294002, 4′-NH2 can be immobilized on an epoxy containing solid surface, which is beneficial for binding studies. Moreover, studies suggest that LY 294002, 4′-NH2 interacts with non-PI 3-kinase cellular proteins such as mTOR, ALDH1, Brd4, GSK3β and CKIIα. Another useful characteristic of LY 294002, 4′-NH2 is that it functions as a reversible inhibitor of PI 3-kinase.
1. Huang, M., et al. 2003. J. Pharmacol. Exp. Ther. 304: 753-760. PMID: 12538831 2. Saleh, S.N., et al. 2009. J. Physiol. 587: 5361-5375. PMID: 19770190 3. Moriguchi, A., et al. 2010. Circ. J. 74: 2393-2402. PMID: 20877127
Soluble in DMSO (100 mM).
Store at 4° C
~534.2° C at 760 mmHg (Predicted)
~1.3 g/cm3 (Predicted)
n20D 1.66 (Predicted)
PI 3-kinase p110β: IC50 = 0.10 µM; PI 3-kinase p110α: IC50 = 0.18 µM; PI 3-kinase p110δ: IC50 = 0.23 µM; PI 3-kinase p110γ: IC50 = 1.97 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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LY 294002, 4prime-NH2 Product Citations
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ScheidScheid, MP. et al. (PubMed 9636168) used LY 294002 (4'-NH2), a PI3K inhibitor, to confirm that activation of PKB depends on the activity of PI3K. Cells incubated with LY 294002 were able to completely block PKB activation, even in the presence of activating cytokines. -SCBT Publication Review
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