CAY10505

Uses

CAY10505 is a phosphoinositide 3-kinase gamma (PI3Kγ) specific inhibitor and improves hypertension-associated vascular endothelial dysfunction.

Biological Activity

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]

in vivo

IC 50

PI3Kγ: 30 nM (IC₅₀, Neurons)

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.