Phosphatidylinositol 3-kinase -PI3K) catalyzes the phosphorylation of phosphatidylinositol at the 3 position to produce the second messengers phosphatidylinositol--3,4)-bisphosphate -PtdIns--3,4)-P2) and PtdIns--3,4,5)-P3). Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are 4 isoforms -p110.alpha., p110.beta., p110.delta., and p100.gamma.), and a p85 regulatory subunit. TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110.beta.. Inhibition appears to occur at the ATP binding site based on the observed increase in IC50 from 5 to ~50 nM at ATP concentrations of 50 uM and 1 mM, respectively. TGX-221 inhibits PtdIns--3,4)-P2 production in platelets with an IC50 of 50 nM. Selective inhibition of PI3K p110.beta. results in defective platelet thrombus formation and defines PI3K as a target for antithrombotic therapy.
產(chǎn)品描述
A potent, selective, and cell permable inhibitor of PI3K p110b; IC50 increases from 5 to ~50 nM at ATP concentrations of 50 uM and 1 mM, respectively; inhibits PtdIns--3,4)-P2 production in platelets with an IC50 value of 50 nM