1596348-32-1

Usage

Uses

KDOAM 21 is an inhibitor to KDM5A (Lysine Demethylase 5A) which is a protein coding gene.

Upstream product

• 41438-38-4 diethyl pyridine-2,4-dicarboxylate 
• 499-80-9 pyridine-2,4-dicarboxylic acid 
• 21908-08-7 ethyl 2-formylpyridine-4-carboxylate 
• 123-83-1 N'-ethyl-N,N-dimethyl-1,2-ethanediamine 

Relevant academic research and scientific papers

HISTONE DEMETHYLASE 5 INHIBITORS AND USES THEREOF

Provided herein are compounds of Formulae (I) and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the compounds or compositions disclosed herein for treating and/or preventing proliferative diseases, cancers, carcinoma lung cancer, breast cancer, liver cancer, pancreatic cancer, gastric cancer, ovarian cancer, colon cancer, colorectal cancer, leukemia, sarcoma and/or cardiovascular diseases in a subject in need thereof. In certain embodiments, the sarcoma is Ewing's sarcoma. Provided are methods of inhibiting a histone demethylase in a subject and/or in a cell, tissue, or biological sample. In certain embodiments, the histone demethylase is a KDM. In certain embodiments, the KDM is KDM5. In certain embodiments, the biological sample is a cell. In certain embodiments, the biological sample is a tissue.

INHIBITORS OF HISTONE DEMETHYLASES

The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form (I).

INHIBITORS OF HISTONE DEMETHYLASES

Compounds of the form In which Q is selected from -CH=NR12, –W, -CH=2NHR13, –CH=O and -CH(OR17)2 capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.