LY294002

LY294002

LY294002 is a molecule that acts as a specific inhibitor of phosphoinositide 3-kinases (PI3Ks). It was first synthesized and studied by scientists at the Eli Lilly and Company in the 1990s. LY294002 has been widely used in cell biology and cancer research to understand the role of PI3Ks and the PI3K/AKT/mTOR pathway in cell growth, proliferation, and survival.

Chemistry

LY294002 is a synthetic molecule that belongs to the class of morpholine derivatives. It is a quinoline derivative with a morpholine ring attached to the quinoline nucleus at the 4-position. The chemical formula of LY294002 is C19H17NO3.

Mechanism of Action

LY294002 inhibits PI3Ks by binding to the ATP-binding pocket of these enzymes, thereby preventing the phosphorylation of phosphatidylinositol (4,5)-bisphosphate (PIP2) to phosphatidylinositol (3,4,5)-trisphosphate (PIP3). This inhibition disrupts the activation of AKT, a downstream effector of PI3K, and thus blocks the PI3K/AKT/mTOR pathway.

Applications in Research

LY294002 has been extensively used in research to study the role of the PI3K/AKT/mTOR pathway in various biological processes and diseases. It has been particularly useful in cancer research, where the PI3K/AKT/mTOR pathway is often dysregulated. By using LY294002, researchers have been able to elucidate the roles of this pathway in cell growth, proliferation, survival, and apoptosis.

Safety and Toxicity

While LY294002 is a valuable tool in research, it is not suitable for use in humans due to its toxicity. It has been found to cause liver damage in animal studies. Therefore, the use of LY294002 is limited to in vitro and animal studies.

See Also

• Phosphoinositide 3-kinase
• PI3K/AKT/mTOR pathway
• Cancer research

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