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2448475-08-7

中文名稱 KDOAM-25 (citrate)
英文名稱 KDOAM-25 (citrate)
CAS 2448475-08-7
2448475-08-7 結(jié)構(gòu)式 2448475-08-7 結(jié)構(gòu)式

基本信息

中文別名
化合物 T11750
英文別名
KDOAM-25 (citrate)

物理化學(xué)性質(zhì)

形態(tài)Solid
顏色Light yellow to yellow

常見問題列表

生物活性
KDOAM-25 citrate 是有效,高選擇性的組蛋白賴氨酸脫甲基酶 5 (KDM5) 抑制劑,對(duì) KDM5A,KDM5B,KDM5C,KDM5D 的 IC50 分別為 71 nM,19 nM,69 nM,69 nM。KDOAM-25 citrate 可增加轉(zhuǎn)錄起始位點(diǎn)的整體 H3K4 甲基化,并損害多發(fā)性骨髓瘤 MM1S 細(xì)胞的增殖。
靶點(diǎn)

IC50: 71 nM (KDM5A), 19 nM (KDM5B), 69 nM (KDM5C), 69 nM (KDM5D)

體外研究

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 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 IC 50 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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