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). It alters the differentiation of bone marrow cells, augmenting GM-CSF-induced development into subsets of mature and immature dendritic cells. Inverse agonists of PPARβ/δ, including DG-172, inhibit cancer cell invasion through suppression of ANGPTL4 expression.
[1]. lieber s, scheer f, meissner w, et al. (z)-2-(2-bromophenyl)-3-{[4-(1-methyl-piperazine)amino]phenyl}acrylonitrile (dg172): an orally bioavailable pparβ/δ-selective ligand with inverse agonistic properties. j med chem. 2012 mar 22;55(6):2858-68.
[2]. lieber s, scheer f, finkernagel f, et al. the inverse agonist dg172 triggers a pparβ/δ-independent myeloid lineage shift and promotes gm-csf/il-4-induced dendritic cell differentiation. mol pharmacol. 2015 feb;87(2):162-73.
[3]. adhikary t, brandt dt, kaddatz k, et al. inverse pparβ/δ agonists suppress oncogenic signaling to the angptl4 gene and inhibit cancer cell invasion. oncogene. 2013 oct 31;32(44):5241-52.
