LY294002

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LY294002
Ly294002.png
Identifiers
CAS number 154447-36-6 YesY
PubChem 3973
ChemSpider 3835 N
ChEMBL CHEMBL98350 N
Jmol-3D images Image 1
Properties
Molecular formula C19H17NO3
Molar mass 307.34 g mol−1
Except where noted otherwise, data are given for materials in their standard state (at 25 °C (77 °F), 100 kPa)
 N (verify) (what is: YesY/N?)
Infobox references

LY294002 is a morpholine-containing chemical compound that is a potent inhibitor of phosphoinositide 3-kinases (PI3Ks).[1] 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 1.4 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.[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]

LY294002 is also a BET-bromodomain inhibitor.[5]


Application[edit]

Research[edit]

It has been shown that LY294002 administration has an additive effect on quercetin antiviral activity against hepatitis C virus. [6]


References[edit]

  1. ^ Maira et al. (2009). "PI3K inhibitors for cancer treatment: where do we stand?". doi:10.1042/BST0370265. 
  2. ^ "Card for LY294002 in DrugBank". DrugBank. Retrieved 2009-09-25. 
  3. ^ Chris J. Vlahos et al. (1994). "A Specific Inhibitor of Phosphatidylinositol 3-Kinase, 2-(4-Morpholinyl)-8-phenyl-4H-l-benzopyran-4-one (LY294002)". Journal of Biological Chemistry 269 (7): 5241–5248. PMID 8106507. 
  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. 
  5. ^ Dittmann, Antje; Werner, Thilo; Chung, Chun-Wa; Savitski, Mikhail M.; Fälth Savitski, Maria; Grandi, Paola; Hopf, Carsten; Lindon, Matthew; Neubauer, Gitte; Prinjha, Rabinder K.; Bantscheff, Marcus; Drewes, Gerard (2013). "The Commonly Used PI3-Kinase Probe LY294002 is an Inhibitor of BET Bromodomains". ACS Chemical Biology: 131210150813004. doi:10.1021/cb400789e. 
  6. ^ Pisonero-Vaquero S (Mar 2014). "Modulation of PI3K-LXRα-dependent lipogenesis mediated by oxidative/nitrosative stress contributes to inhibition of HCV replication by quercetin.". Lab Invest. 94 (3): 262–274. PMID 24492281.