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GW501516 (GSK-516, GW1516) is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. The PPARβ/δ agonist GW501516 inhibited the increase caused by TNF-α in the mRNA levels of the NF-κB target genes interleukin 8 (IL-8), TNF-α and thymic stromal lymphopoietin (TSLP). GW501516 exhibited agonist effects with EC(50) values of 560 and 55 nM against PPARα and PPARδ, respectively, in a luciferase assay. Moreover, GW501516 also exhibited potent ability to induce oleic acid oxidation in a human myotube cell assay with EC(50)=3.7 nM. In contrast, GW501516 treatment decreased TNF-α-induced p65 acetylation. GW501516 increased AMPK phosphorylation and the subsequent p300 phosphorylation, leading to a marked reduction in the association between p65 and this transcriptional co-activator.
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Source | Oncotarget (2017). Figure 1. GW501516 |
| Method | migration assay | |
| Cell Lines | MDA-MB-231, MDA-MB-435, and ZR-75-1 cells | |
| Concentrations | 100 nM | |
| Incubation Time | 48 h | |
| Results | Consistent with the results in MDA-MB-231 cells, the migration of other high metastatic human breast cancer cell lines MDA-MB-435 and ZR-75-1 was dose-dependently inhibited in the presence of GW501516 |
| Molecular Weight | 453.5 |
| Formula | C21H18F3NO3S2 |
| CAS Number | 317318-70-0 |
| Solubility (25°C) | DMSO 47 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PPAR Products |
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| Amorfrutin B
Amorfrutin B is a highly potent natural peroxisome proliferation-activated receptor γ (PPARγ) agonist with oral activity with Ki values of 19 nM and EC50 values of 73 nM, respectively. |
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