RSM-932A is a selective inhibitor of choline kinase α (CHOKα; IC50s = 1 and >50 μM for CHOKα and β, respectively). It induces apoptosis via CHOP signaling and endoplasmic reticulum (ER) stress in MDA-MB-231, MCF-7, SW620, and H460 cancer cells, but it only induces cell cycle arrest and not apoptosis in NCM460 and MCF-10A normal epithelial cells. RSM-932A inhibits the growth of HT-29 colon cancer cells in vitro (IC50 = 1.15 μM) and in vivo in a mouse xenograft model (ED50 = 7.5 mg/kg).
