Preferred Label : NSD2 Inhibitor KTX-1001;
NCIt synonyms : MMSET Inhibitor KTX-1001; WHSC1 Inhibitor KTX-1001;
NCIt definition : An orally available small molecule inhibitor of the histone-lysine N-methyltransferase
nuclear receptor-binding SET domain protein 2 (NSD2; MMSET; WHSC1), with potential
antineoplastic activity. Upon oral administration, NSD2 inhibitor KTX-1001 selectively
targets and binds to NSD2, and inhibits its catalytic activity and the mono- and di-methylation
of histone H3 lysine 36 (H3K36). This modulates the expression of genes involved in
cellular processes including cellular proliferation, which may lead to decreased growth
of cancer cells. NSD2, a member of the NSD family of histone lysine methyltransferase
enzymes that catalyzes the mono- and di-methylation of H3K36, is overexpressed and
dysregulated in many types of cancers.;
Molecule name : KTX-1001; KTX 1001;
NCI Metathesaurus CUI : CL1906219;
Origin ID : C199280;
concept_is_in_subset
- has_target
