KDOAM-25 (citrate)

IC50: 71 nM (KDM5A), 19 nM (KDM5B), 69 nM (KDM5C), 69 nM (KDM5D)

KDOAM-25 citrate inhibits most potently KDM5B with an IC ₅₀ of ∼50 μM and the other KDM5 family members at concentrations above 100 μM. KDOAM-25 citrate shows no cellular activity on any of the other tested JmjC family members.
KDOAM-25 citrate is able to reduce the viability of MM1S cells with an IC ₅₀ of ∼30 μM after a delay of 5-7 days.
KDOAM-25 citrate 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.
KDOAM-25 citrate (50 μM) increases with approximately twice as much H3K4me3 in in multiple myeloma cells.