Preferred Label : PI3K/BET Inhibitor LY294002;
NCIt synonyms : 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one; 2-Morpholin-4-yl-8-phenylchromen-4-one; 4H-1-Benzopyran-4-one, 2-(4-morpholinyl)-8-phenyl-;
NCIt related terms : LY-294002;
NCIt definition : A morpholine-based inhibitor of phosphatidylinositol 3-kinase (PI3K) and the bromodomain
and extra-terminal (BET) family of proteins, with potential antineoplastic activity.
Upon administration, the PI3K/BET inhibitor LY294002 specifically targets and binds
to both PI3K and the acetylated lysine recognition motifs in the bromodomains of BET
proteins. Inhibition of PI3K activity inhibits the PI3K/AKT kinase signaling pathway.
This may result in inhibition of growth and survival for tumor cells in which the
PI3K-mediated signaling pathway is overactivated. Inhibition of BET proteins prevents
their interaction with acetylated histones, disrupts chromatin remodeling and inhibits
the expression of oncogenic drivers that are important for cell proliferation and
survival, which together may lead to an inhibition of proliferation in BET-overexpressing
tumor cells. Activation of the PI3K signaling pathway is frequently associated with
tumorigenesis. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional
regulators and play an important role during development and cellular growth. In tumor
cells, BET proteins play a key role in the regulation of oncogene transcription and
tumor cell proliferation.;
UNII : 31M2U1DVID;
CAS number : 154447-36-6;
Molecule name : LY 294002; LY-294002;
NCI Metathesaurus CUI : CL550844;
Origin ID : C148229;
UMLS CUI : C0251991;
Automatic exact mappings (from CISMeF team)
- Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
