KDM-IN-6

Names

[ Name ]:
KDM-IN-6

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Demethylase

[Target]

IC50: 0.16 μM (KDM2A)[1]

[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[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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₃H₃₈N₄O

[ Molecular Weight ]:
506.68

[ Storage condition ]:
-20°C

Related Compounds

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