Stemcell, 100-1651, AG-14361

Augment the effectiveness of chemotherapeutic agents in cancer cells with AG-14361, a selective, competitive inhibitor of poly (ADP-ribose) polymerase 1 (PARP1; Ki = 6.3 nM). PARP1 is a nuclear enzyme critically involved in DNA repair pathways. When activated by DNA damage, PARP1 catalyzes the production of poly (ADP-ribose) using nicotinamide adenine dinucleotide (NAD+) as a substrate (Ray Chaudhari & Nussenzweig. Nat Rev Mol Cell Biol, 2017). AG-14361 competes with NAD+ to bind to the catalytic site of PARP1, inhibiting the enzyme’s activity (Calabrese et al. JNCI J Natl Cancer Inst, 2004).

AG-14361 has been used for:

CANCER RESEARCH

· Enhance the activity of chemotherapeutic agents and radiation therapy in a number of human cancer cell lines (Calabrese et al. JNCI J Natl Cancer Inst, 2004; De Soto et al. J Clin Oncology, 2010; Smith et al. Clin Cancer Res, 2005).

· Provoke complete tumor regression, in combination with temozolomide, in a mouse xenograft model of colon cancer (Calabrese et al. JNCI J Natl Cancer Inst, 2004).