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GSK2033

Catalog No. T15427   CAS 1221277-90-2

GSK2033 is an antagonist of LXR (pIC50s: 7 and 7.4 for LXRα or LXRβ, respectively).

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GSK2033 Chemical Structure
GSK2033, CAS 1221277-90-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 44.00
5 mg In stock $ 97.00
10 mg In stock $ 163.00
25 mg In stock $ 270.00
50 mg In stock $ 432.00
100 mg In stock $ 693.00
500 mg In stock $ 1,560.00
1 mL * 10 mM (in DMSO) In stock $ 127.00
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Purity: 99.05%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK2033 is an antagonist of LXR (pIC50s: 7 and 7.4 for LXRα or LXRβ, respectively).
Targets&IC50 LXRβ:7.4(pic50), LXRα:7 (pic50)
In vitro GSK2033 dose-dependently inhibits basal transcription in full-length LXRα or full-length LXRβ cotransfection assays (IC50s: 17 nM and 9 nM, respectively). GSK2033 also effectively inhibits the transcription of an ABCA1 driven luciferase reporter dose-dependently (IC50s: 52 nM for LXRα and 10 nM for LXRβ). GSK2033 also suppresses the expression of both of fatty acid synthase (FASN) and SREBP1[2].
In vivo GSK2033 (one month) treatment, does not have obviously effects on hepatic triglyceride levels. GSK2033 treatment also have no effects on plasma triglyceride levels[2].
Molecular Weight 591.66
Formula C29H28F3NO5S2
CAS No. 1221277-90-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (50.70 mM), Sonication and heating are recommended.

TargetMolReferences and Literature

1. Zuercher WJ, et al. Discovery of tertiary sulfonamides as potent liver X receptor antagonists. J Med Chem. 2010 Apr 22;53(8):3412-6. 2. Griffett K, et al. Promiscuous activity of the LXR antagonist GSK2033 in a mouse model of fatty liver disease. Biochem Biophys Res Commun. 2016 Oct 21;479(3):424-428.

TargetMolCitations

1. Liu Y, Wang Z, Jin H, et al.Squalene-epoxidase-catalyzed 24 (S), 25-epoxycholesterol synthesis promotes trained-immunity-mediated antitumor activity.Cell Reports.2024, 43(4).

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Metabolism Compound Library Bioactive Compound Library Nuclear Receptor Compound Library Bioactive Compounds Library Max

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Keywords

GSK2033 1221277-90-2 Metabolism Liver X Receptor Liver X receptor Inhibitor inhibit LXR GSK-2033 GSK 2033 inhibitor

 

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