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DG-172 is an orally available inverse agonist of PPARβ/δ (IC50 = 27 nM), down-regulating transcription of ANGPTL4 in mouse myoblasts (IC50 = 9.5 nM).1 It alters the differentiation of bone marrow cells, augmenting GM-CSF-induced development into subsets of mature and immature dendritic cells.2 Inverse agonists of PPARβ/δ, including DG-172, inhibit cancer cell invasion through suppression of ANGPTL4 expression.3
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1. (Z)-
2. The inverse agonist DG172 triggers a PPARβ/δ-
3. Inverse PPARβ/δ agonists suppress oncogenic signaling to the ANGPTL4 gene and inhibit cancer cell invasion. Oncogene 32(44), 5241-5252 (2013).