LY294002 is a
morpholine
Morpholine is an Organic compound, organic chemical compound having the chemical formula oxygen, O(carbon, Chydrogen, H2CH2)2nitrogen, NH. This heterocycle features both amine and ether functional groups. Because of the amine, morpholine is a bas ...
-containing chemical compound that is a potent inhibitor of numerous proteins, and a strong inhibitor of
phosphoinositide 3-kinase
Phosphoinositide 3-kinases (PI3Ks), also called phosphatidylinositol 3-kinases, are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which i ...
s (PI3Ks).
It is generally considered a non-selective research tool, and should not be used for experiments aiming to target PI3K uniquely.
Two of these are the proto-oncogene serine/threonine-protein kinase (
PIM1) and the
phosphatidylinositol-4,5-bisphosphate 3-kinase P110 gamma, catalytic subunit gamma isoform.
With an
IC50 of 1.4 μM it is somewhat less potent than
wortmannin, another well-known
PI3 kinase inhibitor. However, LY294002 is a reversible inhibitor of PI3K whereas wortmannin acts irreversibly.
Application of LY294002 causes a substantial acceleration of
MEPP frequency (150 μM) at the frog neuromuscular junction through a mechanism that is independent of intraterminal calcium. LY294002 causes the release of MEPPs through a perturbation of synaptotagmin function.
LY294002 is also a
BET inhibitor
BET inhibitors are a class of drugs that reversibly bind the bromodomains of Bromodomain and Extra-Terminal motif (BET) proteins BRD2, BRD3, BRD4, and BRDT, and prevent protein-protein interaction between BET proteins and acetylated histones a ...
(e.g. of BRD2, BRD3, and BRD4).
Application
Research
It has been shown that LY294002 administration has an additive effect on
quercetin
Quercetin is a plant flavonol from the flavonoid group of polyphenols. It is found in many fruits, vegetables, leaves, seeds, and grains; capers, red onions, and kale are common foods containing appreciable amounts of it. It has a bitter flavor ...
antiviral activity against
hepatitis C virus
The hepatitis C virus (HCV) is a small (55–65 nm in size), enveloped, positive-sense single-stranded RNA virus of the family ''Flaviviridae''. The hepatitis C virus is the cause of hepatitis C and some cancers such as liver cancer ( hepatoc ...
.
References
{{reflist
4-Morpholinyl compounds
Chromones
Phosphoinositide 3-kinase inhibitors