KDOAM-25 citrate (C09-1141-480)

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. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cellsIn VitroKDOAM-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. ?/nKDOAM-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. ?/nKDOAM-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. ?/nKDOAM-25 citrate (50 μM) increases with approximately twice as much H3K4me3 in in multiple myeloma cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:KDM5. Specification: 0.98 Molecular Formula: C21H33N5O9 Molecular Weight: 499.51