Fig. 2: STL1267 regulates REV-ERB target genes in cell-based assays.
From: Structural basis of synthetic agonist activation of the nuclear receptor REV-ERB
a HepG2 cells treated with DMSO (blue), SR9009 (purple) or STL1267 (light blue) for 24 h (n = 3 to 8) followed by assessment of cell viability by crystal violet staining. DMSO vs. 10 μM SR9009. b Proliferating C2C12 cells treated with DMSO (blue) SR9009 (purple) or STL1267 (light blue) for 24 h (n = 3 to 8) followed by assessment of cell viability by crystal violet staining. (DMSO vs. 10 μM SR9009 P = 0.0003; DMSO vs. 20 μM SR9009 P < .0001; DMSO vs. 20 μM STL1267 P = 0.0481). c Expression of BMAL1 in HepG2 cells in response to 24 h treatment with DMSO (blue), 5 μM STL1267 (purple) or SR9009 (light blue) (n = 4) P = 0.0010 vehicle vs. STL1267, P = 0.0009 vehicle vs. SR9009. Relative gene expression in C2C12 cells (n = 3) in response to REV-ERB agonist treatment (5 μM) was assessed for mitochondrial complex genes (Mt-Nd1 – DMSO vs. SR9009 P = 0.0024 and vs. STL1267 P = 0.0001; Mt-Co1 – DMSO vs. STL1267 P = 0.0005) (d), fatty acid oxidation (Vlcad – DMSO vs. SR9009 P = 0.062 and vs. STL1267 P = 0.0074; Lcad – DMSO vs. SR9009 P = 0.0209 and vs. STL1267 P = 0.007; Scad – DMSO vs. SR9009 P = 0.0374 and vs. STL1267 P = 0.0030) (e), and mitochondrial function/biogenesis (Lkb1 – DMSO vs. STL1267 P = 0.0316; Sirt1 – DMSO vs. STL1267 P = 0.0600; Ppargca1 – DMSO vs. SR9009 P = 0.0015 and vs. STL1267 P = 0.0012; Nampt – DMSO vs. SR9009 P = 0.0338 and vs. STL1267 P = 0.0542)(f). *P < 0.05, **P < 0.01, ***P < 0.001 and ****P < 0.0001 vs DMSO or vehicle control by one-way ANOVA followed by Dunnett’s post hoc test. Data are presented as mean ± SEM. Source data are available as a Source Data file.
