产品描述:
(R)-ErSO is an activator of the anticipatory unfolded protein response (a-UPR).{67629} It inhibits protein synthesis and induces intracellular ATP depletion in T47D cells that express estrogen receptor α (ERα), but not MDA-MB-231 cells which lack ERα, when used at a concentration of 1 µM. (R)-ErSO (1 µM) also increases levels of phosphorylated eukaryotic translation initiation factor 2α kinase 3 (EIF2AK3), also known as PERK, eukaryotic translation initiation factor 2α subunit (eIF2α), and AMP-activated protein kinase (AMPK), markers of a-UPR activation, in T47D cells. It is cytotoxic to T47D, TYS, BT474, and ZR-75-1 ERα-positive breast cancer cells (IC50s = 16.4, 11.1, 26.9, and 42.8 nM, respectively). In vivo, (R)-ErSO (40 mg/kg) induces tumor regression in an MCF-7 mouse xenograft model. It also induces tumor regression in an ST941/HI breast cancer patient-derived xenograft (PDX) mouse model.