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编 号:F619074
分子式:C15H25N5O2
分子量:307.39
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生物活性:
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.

体外研究:
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. KDOAM-25 is able to reduce the viability of MM1S cells with an IC50 of ~30 μM after a delay of 5-7 days. 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. KDOAM-25 (50 μM) increases with approximately twice as much H3K4me3 in in multiple myeloma cells.
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