Chemical Name : LY 294002
CAS : 154447-36-6
Synonyms: 4H-1-Benzopyran-4-one, 2-(4-morpholinyl)-8-phenyl
Solubility:Soluble in DMSO
Storage:-20C 2 years
LY 294002 has been shown to be a potent inhibitor of PI 3-kinase activity, acting as a competitive inhibitor for ATP binding site of the enzyme. LY 294002 inhibits cell proliferation of choroidal melanoma OCM-1 cells, the IC50 observed was about 10 µM, a concentration higher than, but compatible with, the one (1.4 µM) reported for in vitro inhibition of PI 3-kinase activity.LY 294002 is also an inhibitor of casein kinase II. Application of LY 294002 causes a substantial acceleration of MEPP frequency (150 µM) at the frog neuromuscular junction, through a mechanism that is independent of intraterminal calcium. LY 294002 causes the release of MEPPs through a perturbation of synaptotagmin function.
1. Tolloczko B, Turkewitsch P, Al-Chalabi M, Martin JG. LY-294002 [2-(4-morpholinyl)- 8-phenyl-4H-1-benzopyran-4-one] affects calcium signaling in airway smooth muscle cells independently of phosphoinositide 3-kinase inhibition. J Pharmacol Exp Ther. 2004 Nov;311(2):787-93. Epub 2004 Jun 11.
2. Zarzy��ska J, Motyl T. Dissimilar effects of LY 294002 and PD 098059 in IGF-I-mediated inhibition of TGF-beta1 expression and apoptosis in bovine mammary epithelial cells. J Physiol Pharmacol. 2005 Jun;56 Suppl 3:181-93.
3. Cory AH, Somerville L, Cory JG. Blockage of cyclin cdk's, PKC and phosphoinositol 3-kinase pathways leads to augmentation of apoptosis in drug-resistant leukemia cells: evidence for interactive effects of flavopiridol, LY 294002, roscovitine, wortmannin and UCN-01. Anticancer Res. 2005 Jan-Feb;25(1A):101-6.