Cell experiment:

The xCELLigence system is used for determining the changes in real time cell proliferation in response to activation of PPARD with an agonist (GW0742) or an inverse agonist (DG172) or the effect of inhibiting ERK signaling in TM4 cells[3].

DG-172 (hydrochloride) is an orally available inverse agonist of PPARβ/δ with IC50 value of 27 nM [1].

Peroxisome proliferator-activated receptors (PPARs) are a member of the class II subset of nuclear receptors. The three PPAR subtypes (PPARα, PPARβ/δ, and PPARγ) regulate their target genes through binding to specific DNA elements (PPREs) as obligatory heterodimers with the retinoid X receptor. PPRE-bound PPARβ/δ complexes have functions in both transcriptional repression and transcriptional activation [1].

DG-172 is a novel PPARβ/δ-selective ligand and an orally available PPARβ/δ inverse agonist with IC50 value of 27 nM. In a cell-based assay, DG-172 efficiently antagonized ligand activation of PPARβ/δ. In C2C12 mouse myoblasts, DG-172 inhibited the expression of PPARβ/δ target gene Angptl4 with IC50 value of 9.5 nM. In WPMY-1 human myofibroblasts, DG-172 induced an enhanced recruitment of HDAC3 to the ANGPTL4 gene [1]. DG172 strongly increased GM-CSF-induced differentiation of primary BMCs into two specific populations, mature and immature dendritic cells (DCs) [2]. DG172 strongly inhibited the serum- and transforming growth factor b (TGFb)-induced invasion of MDA-MB-231 human breast cancer cells into a three-dimensional matrigel matrix [3].

References:
[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.