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KDOAM-25 citrate

CAS No. :

MCE 站：KDOAM-25 citrate

产品活性：KDOAM-25 citrate 是有效，高选择性的组蛋白赖氨酸脱甲基酶 5 (KDM5) 抑制剂，对 KDM5A，KDM5B，KDM5C，KDM5D 的 IC₅₀ 分别为 71 nM，19 nM，69 nM，69 nM。KDOAM-25 citrate 可增加转录起始位点的整体 H3K4 甲基化，并损害多发性骨髓瘤 MM1S 细胞的增殖。

研究领域：Epigenetics

作用靶点：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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