KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC 50 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.
性状
Solid
IC50 & Target[1][2]
IC50: 0.16?μM (KDM2A)
体外研究(In Vitro)
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.KDM2A/7A-IN-1 (0.4, 3.1, 6.2 μM) augments cellular H3K36me2 levels in HeLa cells ectopically expressing catalytically active KDM2A. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 200 mg/mL (394.73 mM; Need ultrasonic)配制储备液