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ChemicalBook--->CAS DataBase List--->2169272-46-0

2169272-46-0

2169272-46-0 Structure

2169272-46-0 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[form ]

Solid
[color ]

Light yellow to yellow
Hazard InformationBack 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]

IC50: 0.16 μM (KDM2A)

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