KDM2A/7A-IN-1 是一种首创、选择性、细胞通过性的组蛋白赖氨酸去甲基化酶 KDM2A/7A 抑制剂，对 KDM2A 的 IC50 值为 0.16?μM，对其选择性是对其他 JmjC 赖氨酸去甲基化酶的 75 倍，同时对甲基转移酶和组蛋白乙酰转移酶无作用。
CAS：2169272-46-0
分子式：C33H38N4O
分子量：506.68
纯度：98%
存储：Store at -20°C

Background:

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.