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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
PPARβ/δ
Available Sizes
Frequently Asked Questions
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