CAY10505

CAY10505 is a potent and selective PI3Kγ inhibitor (IC50= 30 nM)

PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt/mTOR pathway.

In neurons treated with 3.5 μM BA, 200 nM CAY10505 partially reduced the baicalein-induced Akt phosphorylation. [1]

In hypertensive rats, CAY10505 at 0.6 mg.kg-1 p.o. exhibited the following effects 1) effectively reduced MABP; 2) significantly ameliorated vascular endothelium dysfunction in hypertensive rats in combination of DOCA; 3) prominently increased serum nitrite and/or nitrate concentrations.4) prevented hypertension-induced attenuation of ACh-induced endothelium-dependent relaxation.[2]

References:
[1] Tyagi S, Sharma S, Budhiraja RD.  Effect of phosphatidylinositol 3-kinase-γ inhibitor CAY10505 in hypertension, and its associated vascular endothelium dysfunction in rats.  Can J Physiol Pharmacol. 2012 Jul;90(7):881-5.
[2] Sun YY, Lin SH, Lin HC et al.  Cell type-specific dependency on the PI3K/Akt signaling pathway for the endogenous Epo and VEGF induction by baicalein in neurons versus astrocytes. PLoS One.  2013 Jul 19;8(7):e69019.