AV-153 free base, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 free base intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 free base interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 free base has anti-cancer activity[1][2][3].
AV-153 free base causes IC50s for Raji and HL-60 cells of 14.9 mM and 10.3 mM, respectively[1]. AV-153 free base (1 nM to 10 μM; 3 hours) reduces the level of spontaneously arising DNA single-strand breaks (SSBs) in peripheral blood lymphocytes or HL-60 cells by 13-67%[1].
[1]. Nadezhda I Ryabokon, et al. A 1,4-dihydropyridine Derivative Reduces DNA Damage and Stimulates DNA Repair in Human Cells in Vitro. Mutat Res. 2005 Nov 10;587(1-2):52-8. [2]. E Buraka, et al. DNA-binding Studies of AV-153, an Antimutagenic and DNA Repair-Stimulating Derivative of 1,4-dihydropiridine. Chem Biol Interact. 2014 Sep 5;220:200-7. [3]. Lidija Milkovic, et al. Antioxidative 1,4-Dihydropyridine Derivatives Modulate Oxidative Stress and Growth of Human Osteoblast-Like Cells In Vitro. Antioxidants (Basel). 2018 Sep 19;7(9):123.