SLU-PP-915

SLU-PP-915 is a pan-ERR (oestrogen-related receptor) agonist that activates ERRα, ERRβ and ERRγ (EC₅₀ ≈ 400 nM). SLU-PP-915 enhances ERR-mediated transcriptional activity and promotes the expression of genes associated with mitochondrial function and oxidative metabolism; it can be used in research into energy metabolism-related diseases such as heart failure and metabolic syndrome.

Method: Neonatal rat ventricular myocytes (NRVMs) were treated with SLU-PP-915 (10 μM) for 72 h, and RNA-seq transcriptomic analysis was performed to detect changes in gene expression.
Result: SLU-PP-915 treatment induced 602 upregulated and 1521 downregulated genes in NRVMs. Upregulated genes were enriched in fatty acid metabolism, oxidative phosphorylation, and cardiac contraction pathways, while downregulated genes were enriched in cell cycle and developmental pathways^[2].
Method: Neonatal rat ventricular myocytes (NRVMs) were treated with SLU-PP-915 (10 μM) for 24 h. ERK1/2 phosphorylation levels were detected by Western blot, and NFAT transcriptional activity was assessed by NFAT luciferase reporter assay.
Result: SLU-PP-915 mildly induced ERK1/2 phosphorylation at baseline but did not block phenylephrine-induced enhancement of ERK1/2 phosphorylation; moreover, SLU-PP-915 did not inhibit phenylephrine-induced NFAT transcriptional activation^[2].
Method: Neonatal rat ventricular myocytes (NRVMs) were treated with SLU-PP-915 (10 μM) for 72 h. LC3-II and p62 protein levels were detected by Western blot, and autophagic flux was assessed by treatment with bafilomycin.
Result: SLU-PP-915 treatment increased LC3-II and p62 protein levels, and both were further elevated upon bafilomycin treatment, suggesting that SLU-PP-915 induces autophagy in cardiomyocytes^[2].

Method: In a mouse model of MLL-rearranged leukemia, Menin-MLL inhibitor 19 was administered, and its in vivo anti-leukemic efficacy was evaluated by assessing tumor burden and survival.
Result: Menin-MLL inhibitor 19 exhibited dose-dependent tumor growth inhibition in the mouse model and effectively prolonged the survival of mice bearing MLL-rearranged leukemia, providing in vivo evidence for its efficacy as an antitumor drug candidate^[1].