Fig. 1: Characterization of S2L cytotoxicity, uptake, and effect on free cholesterol across multiple cancers.
From: Cytotoxic sigma-2 ligands trigger cancer cell death via cholesterol-induced-ER-stress
a Schematic diagram depicting the structure and functions of different components of the azabicyclononane class of S2L. b Proliferation curves of pancreatic (AsPC-1, HPAC, MIAPaCa-2, KP2), ovarian (OVCAR-8), and synovial sarcoma (SYO-1) cell lines treated with various S2L for 24 h. Data represents mean ± SD; n = 3. Flow cytometry measuring C10-NBD [100 nM, 30 min] fluorescence after incubation at 4 °C (n = 9) (c) or pretreatment with pitstop-2 (n = 6) (d). Data represent mean ± SD. e Representative confocal microscopy images from HPAC cells treated with 100 nM C10-NBD for 20 min counterstained for lysosome. Scale bar equals 20 µm. f Representative confocal microscopy images from AsPC-1 cells treated with 10 µM various compounds for 24 h, stained with filipin and counterstained for lysosome. Scale bar equals 10 µm. Bar graph quantifying count of filipin puncta per µm2 in AsPC-1 (seen in f), HPAC, MiaPaCa-2, and KP2 in a cellular model treated with 10 µM of S2L for 24 h (g) and a mouse model C57BL6/KP2 treated with 60 mg/kg C10 for 21 days (h). Data represent mean ± SD (n = 10 cells). ns not significant; **p < 0.01; ****p ≤ 0.0001.
