DG172 (dihydrochloride)

DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC50 of 27 nM.

Product Specifications

CAS Number

[1361504-77-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

PPAR

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/DG172-dihydrochloride.html

Purity

99.51

Solubility

10 mM in DMSO|H2O : 14.29 mg/mL (ultrasonic)

Smiles

BrC(C=CC=C1)=C1/C(C#N)=C/C(C=C2)=CC=C2N3CCN(C)CC3.[H]Cl.[H]Cl

Molecular Formula

C20H22BrCl2N3

Molecular Weight

455.22

Precautions

H302, H315, H319, H335

References & Citations

[1]Lieber S, 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, 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]Yao PL, et al. Peroxisome Proliferator-activated Receptor-D (PPARD) Coordinates Mouse Spermatogenesis by Modulating Extracellular Signal-regulated Kinase (ERK) -dependent Signaling. J Biol Chem. 2015 Sep 18;290 (38) :23416-31.