产品描述:
Phosphatidylinositol 3-kinase (PI3K) catalyzes the synthesis of the second messengers PtdIns-(3)-P, PtdIns-(3,4)-P2, and PtdIns-(3,4,5)-P3. The PI3K family of enzymes is comprised of 15 members that are divided into three classes according to their structure, substrate specificity, and mode of regulation.{14311} In the class I PI3Ks, p110α is the primary PI3K isoform required for insulin signaling in adipocytes and myotubes and is frequently mutated in primary tumors.{14312} Small molecule inhibitors of p110α are of interest in cancer treatment research. PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM.{14312} It inhibits p110γ and p110β considerably less effectively with IC50 values of 0.076 µM and 1.3 µM, respectively.{14312} In adipocytes and myotubes, PIK-75 blocks production of PIP2 and/or PIP3, phosphorylation of Akt, and activation of mTORC1.{14312}