KDOAM-25

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KDOAM-25（KDM5 抑制剂 KDOAM 25）是一种有效的、选择性的 KDM5 亚家族 (JARID1) 抑制剂。

KDOAM-25 (KDM5 inhibitor KDOAM 25) is a potent, selective KDM5 sub-family(JARID1) inhibitor with biochemical IC50 of 71/19/69/69 nM for KDM5A/B/C/D, respectively; weakly inhibits KDM4C/KDM2B (IC50=4.8/4.4 uM) and good selectivity over other demethylases; most potently inhibits KDM5B (IC50=50 uM) and increases H3K4me3 levels in Hela cells; increases global H3K4 methylation, causes G1 cell-cycle arrest and impairs cell proliferation in multiple myeloma MM1S cells.

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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KDM5 inhibitor KDOAM 25

Chromatin/Epigenetic

Histone Demethylase

Histone Demethylase

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2230731-99-2

307.398

C15H25N5O2

>98% (HPLC)

10 mM in DMSO

CCN(CCN(C)C)C(=O)CNCC1=NC=CC(=C1)C(=O)N

2-[[[2-[2-(Dimethylamino)ethyl-Ethyl-Amino]-2-Oxidanylidene-Ethyl]amino]methyl]pyridine-4-Carboxamide

(-20℃)

With Ice Pack

≥ 2 years