(R)-ErSO

(R)-ErSO is an activator of the anticipatory unfolded protein response (a-UPR). It inhibits protein synthesis and induces intracellular ATP depletion in T47D cells that express estrogen receptor alpha (ERalpha), but not MDA-MB-231 cells which lack ERalpha, when used at a concentration of 1 µM. (R)-ErSO (1 µM) also increases levels of phosphorylated eukaryotic translation initiation factor 2alpha kinase 3 (EIF2AK3), also known as PERK, eukaryotic translation initiation factor 2alpha subunit (eIF2alpha), 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 ERalpha-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.Formal Name: (3R)-1,3-dihydro-3-(4-hydroxyphenyl)-3-[4-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)-2H-indol-2-one. CAS Number: 2407860-35-7. Synonyms: ErSO. Molecular Formula: C22H13F6NO3. Formula Weight: 453.3. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble, Methanol: Soluble. SMILES: O=C1[C@@](C(C=C2)=CC=C2OC(F)(F)F)(C(C=C3)=CC=C3O)C4=CC=CC(C(F)(F)F)=C4N1. InChi Code: InChI=1S/C22H13F6NO3/c23-21(24,25)17-3-1-2-16-18(17)29-19(31)20(16,12-4-8-14(30)9-5-12)13-6-10-15(11-7-13)32-22(26,27)28/h1-11,30H,(H,29,31)/t20-/m1/s1. InChi Key: ZFSRXAHDJSCEDS-HXUWFJFHSA-N.