| Identification | Back Directory | [Name]
KDM2A/7A-IN-1 | [CAS]
2169272-46-0 | [Synonyms]
KDM-IN-6
KDM2A/7A-IN-1
1H-Indole-3-carbonitrile, 1-acetyl-2,3-dihydro-3-phenyl-2-[5-[7-(1-pyrrolidinyl)heptyl]-3-pyridinyl]-, (2S,3S)- | [Molecular Formula]
C33H38N4O | [MDL Number]
MFCD32174259 | [MOL File]
2169272-46-0.mol | [Molecular Weight]
506.68 |
| Hazard Information | Back Directory | [Biological Activity]
KDM2A/7A-IN-1 is a first-in-class, selective and cell-passing inhibitor of histone lysine demethylase KDM2A/7A with IC50 value of 0.16 μM for KDM2A It is 75 times more potent than other JmjC lysine demethylases, and has no effect on methyltransferases and histone acetyltransferases. | [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 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. | [target]
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