KDM2A/7A-IN-1

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].

Product Specifications

CAS Number

[2169272-46-0]

UNSPSC

12352005

Target

Histone Demethylase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/kdm2a-7a-in-1.html

Purity

99.94

Solubility

DMSO : 200 mg/mL (ultrasonic)

Smiles

CC(N([C@@H](C1=CN=CC(CCCCCCCN2CCCC2)=C1)[C@@]3(C4=CC=CC=C4)C#N)C5=C3C=CC=C5)=O

Molecular Formula

C33H38N4O

Molecular Weight

506.68

References & Citations

[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.