KDM2A/7A-IN-1 |
| カタログ番号GC36388 |
KDM2A/7A-IN-1 は、ヒストン リジン デメチラーゼ KDM2A/7A のクラス初の選択的細胞透過性阻害剤であり、KDM2A の IC50 は 0.16 μM であり、他の JmjC リジン デメチラーゼよりも 75 倍の選択性を示します。メチルトランスフェラーゼおよびヒストンアセチルトランスフェラーゼに対して不活性です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2169272-46-0
Sample solution is provided at 25 µL, 10mM.
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KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases[1]. IC50: 0.16 μM (KDM2A)[1]
KDM2A/7A-IN-1 ((S,S)-6) is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive to methyl transferases, and histone acetyl transferases[1].KDM2A/7A-IN-1 (0.4, 3.1, 6.2 μM) augments cellular H3K36me2 levels in HeLa cells ectopically expressing catalytically active KDM2A[1].
[1]. Gerken PA, et al. Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7. Angew Chem Int Ed Engl. 2017 Dec 4;56(49):15555-15559.
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