Name | KDM2A/7A-IN-1 |
Synonyms | KDM-IN-6 1H-Indole-3-carbonitrile, 1-acetyl-2,3-dihydro-3-phenyl-2-[5-[7-(1-pyrrolidinyl)heptyl]-3-pyridinyl]-, (2S,3S)- |
CAS | 2169272-46-0 |
Molecular Formula | C33H38N4O |
Molar Mass | 506.68 |
Storage Condition | -20°C |
In vitro study | 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 IC 50 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. |
biological activity | KDM2A/7A-IN-1 is an innovative, selective, the cellular histone lysine demethylase KDM2A/7A inhibitor has an IC50 value of 0.16 μm for KDM2A and is 75 times more selective for other JmjC lysine demethylases, it had no effect on both methyltransferase and histone acetyltransferase. |
Target | IC50: 0.16 μm (KDM2A) |