Preferred Label : Iadademstat;
NCIt synonyms : trans-N1-((1R,2S)-2-Phenylcyclopropyl)-1,4-cyclohexanediamine; 1,4-Cyclohexanediamine, N1-((1R,2S)-2-Phenylcyclopropyl)-, trans-;
NCIt definition : An orally available inhibitor of lysine specific histone demethylase 1 (KDM1A; LSD1),
with potential antineoplastic activity. Upon administration, iadademstat binds to
and inhibits LSD1, a demethylase that suppresses the expression of target genes by
converting the di- and mono-methylated forms of lysine at position 4 of histone H3
(H3K4) to mono- and unmethylated H3K4, respectively. LSD1 inhibition enhances H3K4
methylation and increases the expression of tumor suppressor genes. This may lead
to an inhibition of cell growth in LSD1-overexpressing tumor cells. In addition, LSD1
demethylates mono- or di-methylated H3K9, which increases gene expression of tumor
promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription
of these genes. LSD1, an enzyme belonging to the flavin adenine dinucleotide (FAD)-dependent
amine oxidase family, is overexpressed in certain tumor cells and plays a key role
in in the regulation of gene expression, tumor cell growth and survival.;
UNII : 54T74394F8;
InChIKey : ALHBJBCQLJZYON-ZQDZILKHSA-N;
CAS number : 1431304-21-0;
Molecule name : RO 7051790; RO7051790; ORY-1001; ORY 1001; RG6016; RG 6016;
NCI Metathesaurus CUI : CL521133;
Origin ID : C131908;
UMLS CUI : C5235393;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
