TGX-<wbr/>221

TGX-221

CAT N°: 10007349
Price:

48.00 40.80

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.{8039,12235,13740} Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are 4 isoforms (p110?, p110?, p110?, and p100?), and a p85 regulatory subunit.{13740} TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110?.{13192} Inhibition appears to occur at the ATP binding site based on the observed increase in IC50 value from 5 to ~50 nM at ATP concentrations of 50 µM and 1 mM, respectively. TGX-221 inhibits PtdIns-(3,4)-P2 production in platelets with an IC50 value of 50 nM.{13192} Selective inhibition of PI3K p110? results in defective platelet thrombus formation and defines PI3K as a target for antithrombotic therapy.{13192}

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