Drug intelligence / Profile preview

ly294002

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Small Molecules
01

Overview

LY294002 is a morpholine-containing chemical compound and a potent inhibitor of phosphoinositide 3-kinases (PI3Ks), acting as a non-selective research tool. It is not intended for clinical use but is widely used in laboratory research to study the PI3K/AKT signaling pathway. The compound also inhibits other kinases such as PIM1 and DNA-PKcs and has been shown to act as a BET inhibitor (e.g., BRD2/BRD3/BRD4). It accelerates MEPP frequency at the frog neuromuscular junction through synaptotagmin perturbation. In research settings, it has demonstrated additive effects with quercetin against hepatitis C virus.

Other names
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-oneYXCS-1859CS1859CS 1859LY240092LY-240092LY 240092
02

Targets

DNA-PK (DNA-dependent protein kinase)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)BRD4 (Bromodomain-containing protein 4)BRD3 BD1 (Bromodomain-containing protein 3, bromodomain 1)BRD2 (Bromodomain-containing protein 2)

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