TASIN-1 (1678515-13-3) selectively induces apoptosis in cells with truncations in the adenomatous polyposis coli (APC) gene (but not normal cells or wild type cancer cells), an important multifunctional tumor suppressor gene.1 IC50 = 70nM for DLD1 cell line.? It inhibited cancer cell growth in human tumor xenografts (DLD1 and HT29 tumors) and a genetically engineered mouse model (CPC;Apc) of colorectal cancer.? TASIN-1 induces ER stress-dependent JNK activation with ROS production and AKT inhibition via cholesterol depletion.2
Zhang et al. (2016), Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer; Sci. Transl. Med., 8 361ra140
Zhang et al. (2016), Cholesterol Depletion by TASIN-1 Induces Apoptotic Cell Death through the ER Stress/ROS/JNK Signaling in Colon Cancer Cells; Mol. Cancer Ther., 17 943
