PIK-90

Description: PIK-90 is a novel and potent PI3Kalpha/gamma/delta inhibitor with potential anticancer activity. It inhibits PI3Kalpha/gamma/delta with IC50s of 11 nM/18 nM/58 nM, respectively, and is less potent to PI3Kbeta. PIK-90 also inhibits DNA-PK with IC50 of 13 nM. Studies demonstrated that PIK-90 induced increased levels of secreted IgE at 1 umol/L, while it inhibited IgE production at doses of greater than 2 umol/L. PIk-90 has been reported to block Akt phosphorylation. PIK-90 combined with the CDK2 inhibitor has been demonstrated to induce apoptosis in LN229 PTENWT cells. In addition, PIK-90 combined with siRNA against both CDK1 and CDK2 has shown to induce cell death, whereas PIK-90 combined with siRNA against CDK1 or CDK2 had no apoptotic effect.

References: J Cell Biol. 2006 Jul 31; 174(3):437-45; Proc Natl Acad Sci U S A. 2012 Jul 31; 109(31):12722-7.