LY294002 --- PI3K/BET Dual Inhibitor

Bioss

LY294002 --- PI3K/BET Dual Inhibitor [154447-36-6]

16

Research Use Only

98.0

LY294002 is a potent and selective small molecule PI3K inhibitor, inhibits PI3Kalpha/delta/beta with IC50 of 0.5 microM, 0.57 microM and 0.97 microM, respectively. It is the most widely used PI3K inhibitor to study the role of phosphoinositide 3-kinases in the signal transduction pathways involved in cell migration, proliferation, survival, and metabolism. LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. It is more stable in solution than Wortmannin, and also blocks autophagosome formation. Quantitative chemoproteomic profiling shows that LY294002 inhibits the BET bromodomain proteins BRD2, BRD3, and BRD4 with IC50 ~1-2 microM. It competitively inhibits acetyl-lysine binding of the first but not the second bromodomain of BET proteins in cell extracts. LY294002 provides a starting point for the generation of bromodomain inhibitors tapping the chemical space of kinase antagonists.

-20°C

51202000