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GSK0660 CAS: 1014691-61-2

Category: Inhibitors
Product Name: GSK0660
Cat No: I000126
CAS No: 1014691-61-2
Synonyms: methyl 3-(N-(2-methoxy-4-(phenylamino)phenyl)sulfamoyl)thiophene-2-carboxylate
Molecular Formula: C19H18N2O5S
Molecular Weight: 418.5
SMILES: O=S(NC(C=C1)=C(OC)C=C1NC2=CC=CC=C2)(C3=C(C(OC)=O)SC=C3)=O
InChI: InChI=1S/C19H18N2O5S2/c1-25-16-12-14(20-13-6-4-3-5-7-13)8-9-15(16)21-28(23,24)17-10-11-27-18(17)19(22)26-2/h3-12,20-21H,1-2H3
InChIKey: NDFKBGWLUHKMFY-UHFFFAOYSA-N
Solubility: DMSO: ≥ 49 mg/mL
Target: PPAR
Storage: Store at +4°C
CAS 1014691-61-2,GSK0660
  • Description

GSK0660 is a specific antagonist of PPARβ/δ, also has inverse agonist effects when used alone.
Target: PPARβ/δ
in vitro: GSK0660 differentially regulates 273 transcripts in TNFα-treated cells compared to TNFα alone. GSK0660 blocks the TNFα-induced upregulation of CCL8, a chemokine involved in leukocyte recruitment. GSK0660 blocks the effect of TNFα on the expressions of cytokines involved in leukocyte recruitment, including CCL8, CCL17, and CXCL10 and it may therefore block TNFα-induced retinal leukostasis. [1]

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References

1:Mol Vis. 2015 May 20;21:568-76. eCollection 2015. RNA-seq identifies a role for the PPARβ/δ inverse agonist GSK0660 in the regulation of TNFα-induced cytokine signaling in retinal endothelial cells.Savage SR,McCollum GW,Yang R,Penn JS, PMID: 26015769 PMCID: PMC4443583
Abstract: PURPOSE: The peroxisome proliferator-activated receptor beta/delta (PPARβ/δ) is a transcription factor with roles in metabolism, angiogenesis, and inflammation. It has yet undefined roles in retinal inflammation and diabetic retinopathy (DR). We used RNA-seq to better understand the role of the antagonist and inverse agonist of PPARβ/δ, GSK0660, in TNFα-induced inflammation. Understanding the underlying mechanisms of vascular inflammation could lead to new treatments for DR.METHODS: RNA was isolated from human retinal microvascular endothelial cells treated with a vehicle, TNFα, or TNFα plus GSK0660. RNA-seq was performed with a 50 bp single read protocol. The differential expression was determined using edgeR and gene ontology, and a pathway analysis was performed using DAVID. RNA-seq validation was performed using qRT-PCR using the primers for ANGPTL4, CCL8, NOV, CXCL10, and PDPK1.RESULTS: TNFα differentially regulated 1,830 transcripts, many of which are involved in the cytokine-cytokine receptor interaction, chemokine signaling, and inflammatory response. Additionally, TNFα highly upregulated genes involved in leukocyte recruitment, including CCL5, CX3CL1, and CXCL10. GSK0660 differentially regulated 273 transcripts in TNFα-treated cells compared to TNFα alone. A pathway analysis revealed the enrichment of cytokine-cytokine receptor signaling. In particular, GSK0660 blocks the TNFα-induced upregulation of CCL8, a chemokine involved in leukocyte recruitment.CONCLUSIONS: TNFα regulates several genes related to retinal leukostasis in retinal endothelial cells. GSK0660 blocks the effect of TNFα on the expressions of cytokines involved in leukocyte recruitment, including CCL8, CCL17, and CXCL10 and it may therefore block TNFα-induced retinal leukostasis.


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