KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC 50 s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. Multiple myeloma MM1S cells treated with KDOAM-25 citrate show increased global H3K4 methylation at transcriptional start sites and impaired proliferation [1].

KDM5A:71 nM , KDM5D:69 nM , KDM5B:19 nM , KDM5C:69 nM

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 is inactive against any of the other tested JmjC family members [1]. 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 [1]. 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 [1]. KDOAM-25 citrate (50 μM) increases with approximately twice as much H3K4me3 in in multiple myeloma cells [1].