GSK2033

Name: GSK2033
Brand: MedChemExpress
SKU: HY-108688
Rating: 5.0 (34 reviews)

Cat. No.: HY-108688 Purity: 99.53%: Data Sheet
COA

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GSK2033 is a LXR antagonist with pIC₅₀s of 7 and 7.4 for LXRα or LXRβ, respectively.

For research use only. We do not sell to patients.

CAS No. : 1221277-90-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 34 publication(s) in Google Scholar

Other Forms of GSK2033:

GSK2033 (Standard) Get quote

34 Publications Citing Use of MCE GSK2033

Cell Migration/Invasion Assay

RT-PCR

Cell Imaging/Staining

: GSK2033 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 May 14;23(1):542. [Abstract]; The activated ABCB1 gene expression was down regulated by treatment of cells with the LXR antagonist, GSK2033 (0. 0.01, 0.1, 1 μM, 24 h).

: GSK2033 purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2023 Nov 1:266:115605. [Abstract]; GSK2033 (10 μM) enhanced the expression levels of these genes prompted by EHDPP.

: GSK2033 purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2023 Jun;18(6):1339-1346. [Abstract]; The Transwell migration assay of RAW264.7 cells cultured with ACM from astrocytes stimulated with 1 U/mL thrombin (Thr) for 24 hours, followed by the addition of 100 nM GSK2033, and allowed to migrate for 24 hours. Treatment with GSK2033 significantly inhibited the effects of thrombin-induced 25-HC expression on RAW264.7 cell migration.

: GSK2033 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Sep;42(9):1472-1485. [Abstract]; GSK2033 (50 nM) obviously downregulated the expression of LXRα, ABCA1, and E-cad and upregulated the expression of Vim and MMP-2.

: GSK2033 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Sep;42(9):1472-1485. [Abstract]; GSK2033 (50 nM) resulted in the formation of a decreased number of autophagolysosomes, autophagosomes and lipophagic vesicle-like structures.

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Biological Activity
Protocol
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Description

GSK2033 is a LXR antagonist with pIC₅₀s of 7 and 7.4 for LXRα or LXRβ, respectively.

IC₅₀ & Target

pIC50: 7 (LXRα), 7.4 (LXRβ)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	< 100 nM Compound: 17, GSK-2033	Inhibition of SREBP-1c expression in human HepG2 cells Inhibition of SREBP-1c expression in human HepG2 cells	[PMID: 20345102]
THP-1	IC₅₀	< 100 nM Compound: 17, GSK-2033	Inhibition of ABCA1 expression in human THP1 cells Inhibition of ABCA1 expression in human THP1 cells	[PMID: 20345102]

In Vitro

GSK2033 is a LXR antagonist with pIC₅₀s of 7 and 7.4 for LXRα or LXRβ, respectively. GSK2033 dose-dependently suppresses basal transcription in full-length LXRα or full-length LXRβ cotransfection assays with IC₅₀s of 17 nM and 9 nM, respectively. GSK2033 also effectively suppresses the transcription of an ABCA1 driven luciferase reporter dose-dependently displaying IC₅₀s of 52 nM for LXRα and 10 nM for LXRβ. GSK2033 also suppresses the expression of both of fatty acid synthase (FASN) and SREBP1^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

One month treatment of GSK2033 does not have significant effects on hepatic triglyceride levels. Plasma triglyceride levels are also unaffected by treatment with GSK2033^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

591.66

Formula

C₂₉H₂₈F₃NO₅S₂

CAS No.

1221277-90-2

Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=C(C)C=C(C)C=C1C)(N(CC2=CC=C(C3=CC=CC(S(=O)(C)=O)=C3)C=C2)CC4=CC=C(C(F)(F)F)O4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 11.11 mg/mL (18.78 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6902 mL	8.4508 mL	16.9016 mL
5 mM	0.3380 mL	1.6902 mL	3.3803 mL
10 mM	0.1690 mL	0.8451 mL	1.6902 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 3 mg/mL (5.07 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 3 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 3 mg/mL (5.07 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 3 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.53%

Select Batch:

Data Sheet (278 KB) SDS (396 KB)

COA (253 KB) HNMR (144 KB) RP-HPLC (235 KB) LCMS (235 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

Cell Assay ^[2]	HepG2 cells are maintained in minimal essential medium supplemented with 10% FBS and antibiotics. HepG2 cells are then treated for 24 h with GSK2033 followed by assessment of expression of genes by qPCR^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	21-week old male C57BL6 DIO mice are used. Animals are individually housed and fed a high fat diet (60% kcal/fat diet, 20% carbohydrate) for the duration of the experiment that includes GSK2033 administration for 28 days (30 mg/kg, q. d, i. p.). Body weight and food intake are monitored daily^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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. [Content Brief] [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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6902 mL	8.4508 mL	16.9016 mL	42.2540 mL
	5 mM	0.3380 mL	1.6902 mL	3.3803 mL	8.4508 mL
	10 mM	0.1690 mL	0.8451 mL	1.6902 mL	4.2254 mL
	15 mM	0.1127 mL	0.5634 mL	1.1268 mL	2.8169 mL

GSK2033 Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK20331221277-90-2GSK 2033GSK-2033LXRLiver X receptorInhibitorinhibitorinhibit

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GSK2033

Customer Review

Other Forms of GSK2033:

GSK2033 Related Antibodies

34 Publications Citing Use of MCE GSK2033

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

GSK2033 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

GSK2033 Related Classifications

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Customer Review

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