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Merck
CN

SML4244

GSK0660

new

≥98% (HPLC)

Synonym(s):

3-[[[2-Methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-2-thiophenecarboxylic acid methyl ester, Methyl 3-({[2-(methoxy)-4 phenyl]amino}sulfonyl)-2-thiophenecarboxylate, GSK 0660, GSK-0660

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About This Item

Empirical Formula (Hill Notation):
C19H18N2O5S2
CAS Number:
Molecular Weight:
418.49
MDL number:
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Quality Level

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Biochem/physiol Actions

Potent and selective PPARdelta (PPARbeta) antagonist.
GSK0660 is a potent and selective PPARdelta (PPARbeta) agonist (IC50 = 300 nM against GW1516-induced PPARβ/δ reporter activity; IC50 = 155 nM vs >10 µM for PPARα and PPARγ by GW1516 displacement binding assays). GSK0660 effectively antagonizes PPARβ/δ agonist GW501516 (GW1516)-induced target genes expression in multiple cell types, including HuH7, rat L6 myotubes, and mouse BMDMs (1-10 nM GW1516, 100-1000 nM GSK0660).

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Bibimaryam Khan et al.
European journal of pharmacology, 972, 176565-176565 (2024-04-11)
Blockade of PD-1/PD-L1 immune checkpoint is wildly used for multiple types of cancer treatment, while the low response rate for patients is still completely unknown. As nuclear hormone receptor, PPARδ (peroxisome-proliferator-activated receptor) regulates cell proliferation, inflammation, and tumor progression, while
Barry G Shearer et al.
Molecular endocrinology (Baltimore, Md.), 22(2), 523-529 (2007-11-03)
The identification of small molecule ligands for the peroxisome proliferator-activated receptors (PPARs) has been instrumental in elucidating their biological roles. In particular, agonists have been the focus of much of the research in the field with relatively few antagonists being
Andrea Antonosante et al.
Biological research, 56(1), 27-27 (2023-05-25)
The underlying mechanism of Parkinson's disease are still unidentified, but excitotoxicity, oxidative stress, and neuroinflammation are considered key actors. Proliferator activated receptors (PPARs) are transcription factors involved in the control of numerous pathways. Specifically, PPARβ/δ is recognized as an oxidative

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