GSK0660

Catalog No.S5817 Batch:S581701

Technical Data

Formula	C₁₉H₁₈N₂O₅S₂
Molecular Weight	418.49	CAS No.	1014691-61-2
Solubility (25°C)*	In vitro	DMSO	84 mg/mL (200.72 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (binding assay IC50 = 155 nM; antagonist assay IC50 = 300 nM) and is nearly inactive on PPARα and PPARγ with IC50s above approximately 10 μM.

Targets

PPAR-β/δ ^[1]
(binding assay)

155 nM

In vitro

GSK0660 inhibits HRMEC (human retinal microvascular endothelial cells) proliferation and differentiation^[2].

In vivo

GSK0660 is rapidly cleared and does not accumulate in the blood in vivo^[1]. GSK0660 is efficacious against retinal NV when administered by IVIT or IP injection. Intravitreal injection has the advantages of producing high levels of drug at active sites of neovascular disease, but deleterious side effects are associated with this route of drug administration, including endophthalmitis, cataractogenesis, and glaucoma. Systemic administration could avoid these side effects, but it is hampered by the need for repeated dosing to obtain target concentrations of active drug in diseased tissues. It also needlessly exposes disease-free organs and tissues to active drug^[2].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines HRMECs Concentrations 0.01, 0.1, or 1.0 μM Incubation Time 6 h Method HRMECs were seeded in six-well plates at 2 × 10⁵ cells/well and maintained under standard tissue culture conditions. At 80% confluency, the cells were serum starved for 12 hours, then treated on a background of 0.5% serum-containing vehicle (0.1% DMSO) or PPAR-β/δ agonist GW0742 (0.01, 0.1, or 1.0 μM) or on a background of 2% serum-containing vehicle or PPAR-β/δ antagonist GSK0660 (0.01, 0.1, or 1.0 μM) for 6 hours. Cells were washed twice with cold PBS and total RNA was collected. Total RNA isolated from the culture wells was reverse transcribed. Quantitative RT-PCR was performed.
Animal Study:^{^[2]}	Animal Models Sprague-Dawley rat Dosages 0.2 or 1.0 mg/kg Administration i.p.

Cell Assay:^{^[2]}

Cell lines
HRMECs
Concentrations
0.01, 0.1, or 1.0 μM
Incubation Time
6 h
Method
HRMECs were seeded in six-well plates at 2 × 10⁵ cells/well and maintained under standard tissue culture conditions. At 80% confluency, the cells were serum starved for 12 hours, then treated on a background of 0.5% serum-containing vehicle (0.1% DMSO) or PPAR-β/δ agonist GW0742 (0.01, 0.1, or 1.0 μM) or on a background of 2% serum-containing vehicle or PPAR-β/δ antagonist GSK0660 (0.01, 0.1, or 1.0 μM) for 6 hours. Cells were washed twice with cold PBS and total RNA was collected. Total RNA isolated from the culture wells was reverse transcribed. Quantitative RT-PCR was performed.

Animal Study:^{^[2]}

Animal Models
Sprague-Dawley rat
Dosages
0.2 or 1.0 mg/kg
Administration
i.p.

References

Selleck's GSK0660 has been cited by 5 publications

Blastocyst-Derived Lactic Acid May Regulate S100A6 Expression and Function in Mouse Decidualization via Stimulation of Uterine Epithelial Arachidonic [ Cells, 2024, 13(3):206.]	PubMed: 38334598
Blastocyst-Derived Lactic Acid May Regulate S100A6 Expression and Function in Mouse Decidualization via Stimulation of Uterine Epithelial Arachidonic Acid Secretion [ Cells, 2024, 13(3)206]	PubMed: 38334598
Embryo-derive TNF promotes decidualization via fibroblast activation [ Elife, 2023, 12e82970]	PubMed: 37458359
Embryo-derive TNF promotes decidualization via fibroblast activation [ Elife, 2023, 12e82970]	PubMed: 37458359
RORγ Is a Targetable Master Regulator of Cholesterol Biosynthesis in a Cancer Subtype [ Nat Commun, 2019, 11;10(1):4621]	PubMed: 31604910

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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