2169272-46-0

2169272-46-0 structure

Name: KDM-IN-6
Chemical Name: KDM2A/7A-IN-1
CAS Number: 2169272-46-0
Molecular Formula: C₃₃H₃₈N₄O
Molecular Weight: 506.68
Catalog: Signaling Pathways Epigenetics Histone Demethylase
Create Date: 2019-08-03 20:11:59
Modify Date: 2024-01-19 10:18:29
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].

Name	KDM2A/7A-IN-1

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.