KDOAM-25 trihydrochloride

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KDOAM-25 trihydrochloride 

KDOAM-25 trihydrochloride 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 trihydrochloride 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。

KDOAM-25 trihydrochloride

KDOAM-25 trihydrochloride Chemical Structure

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KDOAM-25 trihydrochloride 的其他形式现货产品:

KDOAM-25 citrate

生物活性

KDOAM-25 trihydrochloride 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 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells[1].

IC50 & Target

IC50: 71 nM (KDM5A), 19 nM (KDM5B), 69 nM (KDM5C), 69 nM (KDM5D)[1]

体外研究
(In Vitro)

KDOAM-25 trihydrochloride inhibits most potently KDM5B with an IC50 of ∼50 μM and the other KDM5 family members at concentrations above 100 μM. KDOAM-25 trihydrochloride shows no cellular activity on any of the other tested JmjC family members[1].
KDOAM-25 trihydrochloride is able to reduce the viability of MM1S cells with an IC50 of ∼30 μM after a delay of 5-7 days[1].
KDOAM-25 trihydrochloride 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[1].
KDOAM-25 trihydrochloride (50 μM) increases with approximately twice as much H3K4me3 in in multiple myeloma cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

416.77

Formula

C15H28Cl3N5O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Tumber A, et al. Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chem Biol. 2017 Mar 16;24(3):371-380.

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