Preferred Label : Veledimex;
NCIt synonyms : Benzoic Acid, 2-Ethyl-3-methoxy-, 2-(3,5-Dimethylbenzoyl)-2-((1R)-1-(1,1-dimethylethyl)butyl)hydrazide;
NCIt definition : An orally bioavailable, small molecule diacylhydrazine-based activator ligand, that
can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible
gene regulation system, the RheoSwitch Therapeutic System (RTS). Upon administration
of veledimex, this agent specifically binds to the EcR located on the separately administered
RTS, which includes two fusions proteins: Gal4-EcR, which contains a modified ecdysone
receptor (EcR) fused with the DNA binding domain of the yeast Gal4 transcription factor,
and VP16-RXR, which contains a chimeric retinoid X receptor (RXR) fused with the transcription
activation domain of the viral protein VP16 of herpes simplex virus type 1 (HSV1).
The fusion proteins form inactive, unstable and unproductive heterodimers in the absence
of veledimex. In the presence of veledimex, the protein heterodimer changes to a stable
conformation, forming an active transcription factor complex, which can bind to the
inducible promoter, thereby allowing the induction of controlled transcription of
the target gene.;
UNII : ASU841TV0X;
InChIKey : LZWZPGLVHLSWQX-XMMPIXPASA-N;
CAS number : 1093130-72-3;
Molecule name : INXN-1001; RG-115932;
NCI Metathesaurus CUI : CL554051;
Origin ID : C152847;
UMLS CUI : C4519079;
Automatic exact mappings (from CISMeF team)
Semantic type(s)
UMLS correspondences (same concept)
concept_is_in_subset