Chemical Name: 3-[[[2-Methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-2-thiophenecarboxylic acid methyl ester
Biological ActivityGSK 0660 is a selective PPARδ antagonist (IC50 values are 0.155, > 10 and ≥ 10 μM at PPARδ, PPARα and PPARγ respectively). Exhibits inverse agonist effects when administered by itself.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Identification and characterization of a selective peroxisome proliferator-activated receptor β/δ (NR1C2) antagonist.
Shearer et al.
PPAR-δ in vascular pathophysiology.
PPAR Res., 2008;:164163
The role of PPARs in the endothelium: Implications for cancer therapy.
Bishop-Bailey and Swales
PPAR Res., 2008;:904851
Citations for GSK 0660
The citations listed below are publications that use Tocris products. Selected citations for GSK 0660 include:
18 Citations: Showing 1 - 10
Identification and characterization of a novel anti-inflammatory lipid isolated from Mycobacterium vaccae, a soil-derived bacterium with immunoregulatory and stress resilience properties.
Authors: Smith Et al.
Psychopharmacology (Berl) 2019;
Retinoic acid inhibits white adipogenesis by disrupting GADD45A-mediated Zfp423 DNA demethylation.
Authors: Wang Et al.
J Mol Cell Biol 2017;9:338
Bladder-cancer-associated mutations in RXRA activate peroxisome proliferator-activated receptors to drive urothelial proliferation.
Authors: Halstead Et al.
Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals.
Authors: Niu Et al.
Drug Des Devel Ther 2015;9:5625
Development of telmis. in the therapy of spinal cord injury: pre-clinical study in rats.
Authors: Lin Et al.
Invest Ophthalmol Vis Sci 2015;9:4709
RNA-seq identifies a role for the PPARβ/δ inverse agonist GSK0660 in the regulation of TNFα-induced cytokine signaling in retinal endothelial cells.
Authors: Savage Et al.
Mol Vis 2015;21:568
Activation of PPAR-δ induces microRNA-100 and decreases the uptake of very low-density lipoprotein in endothelial cells.
Authors: Fang Et al.
Br J Pharmacol 2015;172:3728
Peroxisomes in Different Skeletal Cell Types during Intramembranous and Endochondral Ossification and Their Regulation during Osteoblast Differentiation by Distinct Peroxisome Proliferator-Activated Receptors.
Authors: Qian Et al.
PLoS One 2015;10:e0143439
Mechanisms of Nifedipine-Downregulated CD40L/sCD40L Signaling in Collagen Stimulated Human Platelets.
Authors: Chen Et al.
PLoS One 2015;10:e0127054
Modulation of VEGF-induced retinal vascular permeability by peroxisome proliferator-activated receptor-β/δ.
Authors: Suarez Et al.
Invest Ophthalmol Vis Sci 2014;55:8232
An endoplasmic reticulum stress-initiated sphingolipid metabolite, ceramide-1-phosphate, regulates epithelial innate immunity by stimulating β-defensin production.
Authors: Kim Et al.
Mol Cell Biol 2014;34:4368
Merit of ginseng in the treatment of heart failure in type 1-like diabetic rats.
Authors: Tsai Et al.
Biochem J 2014;2014:484161
Decrease of PPARδ in Type-1-Like Diabetic Rat for Higher Mortality after Spinal Cord Injury.
Authors: Tsai Et al.
PPAR Res 2014;2014:456386
Antiplatelet activity of nifed. is mediated by inhibition of NF-κB activation caused by enhancement of PPAR-β/-γ activity.
Authors: Shih Et al.
Br J Pharmacol 2014;171:1490
PPARβ/δ regulates glucocorticoid- and sepsis-induced FOXO1 activation and muscle wasting.
Authors: Castillero Et al.
PLoS One 2013;8:e59726
Peroxisome proliferator-activated receptor-β/δ regulates angiogenic cell behaviors and oxygen-induced retinopathy.
Authors: Capozzi Et al.
Biomed Res Int 2013;54:4197
Isorhamnetin inhibits proliferation and invasion and induces apoptosis through the modulation of peroxisome proliferator-activated receptor γ activation pathway in gastric cancer.
Authors: Ramachandran Et al.
J Biol Chem 2012;287:38028
Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply.
Authors: Mottillo Et al.
Drug Des Devel Ther 2012;287:25038
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