Overview

BSI-201, also known as iniparib, can interact with the zinc finger domain of poly(ADP-ribose) polymerase 1 (PARP1) in vitro, but fails to inhibit the enzyme (Patel et al.). The nitroso metabolite of BSI-201 is highly reactive and forms non-specific covalent interactions with many cysteine-containing proteins (Liu et al.). BSI-201 has demonstrated anti-proliferative effects in triple-negative breast cancer cells (Chuang et al.; Yin et al.), and early studies indicated that it may be useful in treating early-stage triple-negative and BRCA1/2 mutation-associated breast cancer (O’Shaughnessy et al. 2009); however, its efficacy was later found to be insignificant (O’Shaughnessy et al. 2014).REPROGRAMMING· When used in combination with other small molecules, enables derivation of extended pluripotent stem (EPS) cells from both humans and mice (Yang et al.).CANCER RESEARCH· Inhibits the growth of a subset of triple-negative breast cancer cells (Myc/MDA-231), in combination with cisplatin (Chuang et al.; Yin et al.).