Drug intelligence / Profile preview

A-196

Development stage: Preclinical
Lead developer: AbbVie
Modality: Small Molecules

Overview

A-196 is a potent and selective small molecule inhibitor of the histone methyltransferases SUV420H1 (KMT5B) and SUV420H2 (KMT5C), with IC50 values of 25 nM and 144 nM, respectively. It acts as a substrate-competitive inhibitor for both enzymes, leading to decreased di- and tri-methylation of lysine 20 on histone H4 (H4K20me2/3) in cells. This results in reduced nonhomologous end joining (NHEJ)-mediated DNA repair without affecting homology-directed repair. A-196 is primarily used as a chemical probe to study the role of these methyltransferases in epigenetic regulation and genomic integrity[1][2][4][7].

Other names: 6,7-Dichloro-N-cyclopentyl-4-(4-pyridinyl)-1-phthalazinamine

Targets

KMT5C (Lysine methyltransferase 5C)KMT5B (Histone-lysine N-methyltransferase KMT5B)

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