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KDOAM-25 citrate

CAS No. : 2448475-08-7

產(chǎn)品活性：KDOAM-25 citrate 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 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.

研究領(lǐng)域：Epigenetics

作用靶點(diǎn)：Histone Demethylase

In Vitro: KDOAM-25 citrate inhibits most potently KDM5B with an IC₅₀ 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 IC₅₀ 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.

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