LY294002

LY294002
IUPAC name

2-morpholin-4-yl-8-phenylchromen-4-one
Other names

2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
Identifiers
CAS number 154447-36-6 Y
PubChem 3973
ChEMBL CHEMBL98350 N
Jmol-3D images Image 1
Properties
Molecular formula C19H17NO3
Molar mass 307.343
 N (verify) (what is: Y/N?)
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
Infobox references

LY294002 is a morpholine derivative of quercetin.[1] It is a potent inhibitor of phosphoinositide 3-kinases (PI3Ks). Two of these are the proto-oncogene serine/threonine-protein kinase (PIM1) and the phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform.[2] With an IC50 of 1.4uM 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.[3] 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.[4]

References

  1. ^ Maira et al. (2009). "PI3K inhibitors for cancer treatment: where do we stand?". doi:10.1042/BST0370265. http://www.biochemsoctrans.org/bst/037/0265/0370265.pdf. 
  2. ^ "Card for LY294002 in DrugBank". DrugBank. http://www.drugbank.ca/cgi-bin/getCard.cgi?CARD=DB02656.txt. Retrieved 2009-09-25. 
  3. ^ A Specific Inhibitor of Phosphatidylinositol 3=Kinase, 2-(4-Morpholinyl)-8-phenyl-4H-l-benzopyran-4-(oLnYe2 94002), Chris J. Vlahos et al., JBS. 1994;7:5241-5248
  4. ^ Searl TJ, Silinsky EM. (Dec 2005). "LY 294002 inhibits adenosine receptor activation by a mechanism independent of effects on PI-3 kinase or casein kinase II". Purinergic Signal. 1 (4): 389–94. doi:10.1007/s11302-005-0778-6. PMC 2096559. PMID 18404524. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2096559.