KDOAM-25

KDOAM-25 is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC₅₀s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells^[1]. IC50 & Target: IC50: 71 nM (KDM5A), 19 nM (KDM5B), 69 nM (KDM5C), 69 nM (KDM5D)^[1] In Vitro: KDOAM-25 inhibits most potently KDM5B with an IC₅₀ of ∼50 μM and the other KDM5 family members at concentrations above 100 μM. KDOAM-25 shows no cellular activity on any of the other tested JmjC family members^[1].
KDOAM-25 is able to reduce the viability of MM1S cells with an IC₅₀ of ∼30 μM after a delay of 5-7 days^[1].
KDOAM-25 treatment results in a G1 cell-cycle arrest with an increased proportion of MM1S in G1 and a decrease of the proportion of cells in G2 without an increase in the proportion of cells in the apoptotic sub-G1 phase^[1].
KDOAM-25 (50 μM) increases with approximately twice as much H3K4me3 in in multiple myeloma cells^[1].