RSM-932A is a selective inhibitor of choline kinase α (CHOKα; IC50s = 1 and >50 μM for CHOKα and β, respectively).
CAS：850807-63-5
分子式：C46H38Cl2N4.2Br
分子量：877.5
纯度：98%
存储：Store at -20°C

Background:

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.[2] 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). [1]

Reference:
[1]. Lacal, J.C., and Campos, J.M. Preclinical characterization of RSM-932A, a novel anticancer drug targeting the human choline kinase alpha, an enzyme involved in increased lipid metabolism of cancer cells. Mol. Cancer Ther. 14(1), 31-39 (2015).
[2]. Sanchez-Lopez, E., Zimmerman, T., Gomez del Pulgar, T., et al. Choline kinase inhibition induces exacerbated endoplasmic reticulum stress and triggers apoptosis via CHOP in cancer cells. Cell Death Dis. 4, e933 (2013).