Preferred Label : BRG1/BRM Inhibitor FHD-286;
NCIt synonyms : SMARCA4/SMARCA2 ATPase Inhibitor FHD-286;
NCIt related terms : FHD-286;
NCIt definition : An orally bioavailable, allosteric, small molecule inhibitor of transcription activator
BRG1 (SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily
A member 4; SMARCA4) and BRM (SWI/SNF-related matrix-associated actin-dependent regulator
of chromatin subfamily A member 2; SMARCA2), with potential antineoplastic activity.
Upon oral administration, BRG1/BRM inhibitor FHD-286 targets, binds to, and inhibits
the activity of BRG1 and/or BRM, the primary ATPase components and mutually exclusive
subunits of the BRG1/BRM-associated factor (BAF) complexes. This may lead to the inhibition
of the SWI/SNF chromatin remodeling complex, disrupt chromatin remodeling and gene
expression, and result in the downregulation of oncogenic pathways and the inhibition
of tumor cell proliferation. BAF is an important regulator of transcriptional programs
and gene expression. Mutations in BAF or its transcription factor partners are found
in certain diseases including cancers.;
UNII : QHA5XLA4SA;
Molecule name : FHD-286; FHD 286;
NCI Metathesaurus CUI : CL1662216;
Origin ID : C179408;
UMLS CUI : C5555665;
Semantic type(s)
- concept_is_in_subset
- has_target
