GSK2033
Based on 37 publication(s) in Google Scholar
GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.73%
- No. CAS: 1221277-90-2
- Fòrmula: C29H28F3NO5S2
- Peso molecular:591.66
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) GSK2033
More- Immunity. 2024 May 14;57(5):1087-1104.e7. [Abstract]
- Mol Cell. 2025 Sep 18;85(18):3486-3504.e7. [Abstract]
- Sci Adv. 2022 Jul 15;8(28):eabn5295. [Abstract]
- Cell Death Differ. 2020 Aug;27(8):2433-2450. [Abstract]
- Environ Sci Technol. 2025 Apr 25. [Abstract]
- Cancer Lett. 2023 Jun 28:564:216208. [Abstract]
- Phytomedicine. 2025 Jul:142:156691. [Abstract]
- J Pharm Anal. 2026 Apr 8.
- Acta Pharmacol Sin. 2021 Sep;42(9):1472-1485. [Abstract]
- J Transl Med. 2025 May 14;23(1):542. [Abstract]
- Dev Cell. 2026 Apr 29:S1534-5807(26)00150-4. [Abstract]
- JHEP Rep. 2026 May 5.
- Neural Regen Res. 2023 Jun;18(6):1339-1346. [Abstract]
- Clin Transl Med. 2024 Apr;14(4):e1665. [Abstract]
- Cancer Immunol Res. 2023 Oct 4;11(10):1400-1413. [Abstract]
- Cell Rep. 2021 Jun 15;35(11):109233. [Abstract]
- Brain Behav Immun. 2025 Aug 21:106089. [Abstract]
- Brain Behav Immun. 2021 May:94:111-124. [Abstract]
- Lipids Health Dis. 2025 Sep 29;24(1):296. [Abstract]
- J Ethnopharmacol. 2026 Apr 6:360:121150. [Abstract]
- J Ethnopharmacol. 2024 Aug 20:335:118702. [Abstract]
- J Ethnopharmacol. 2024 Jul 16:334:118545. [Abstract]
- Ecotoxicol Environ Saf. 2023 Nov 1:266:115605. [Abstract]
- Eur J Pharmacol. 2023 Jul 5:950:175771. [Abstract]
- Int Immunopharmacol. 2025 Sep 23:162:115189. [Abstract]
- Int J Mol Sci. 2023 Mar 22;24(6):5992. [Abstract]
- Biogerontology. 2025 Jan 31;26(2):49. [Abstract]
- J Cell Mol Med. 2020 Mar;24(6):3384-3398. [Abstract]
- J Inflamm Res. 2025 Oct 1:18:13575-13592. [Abstract]
- ACS Infect Dis. 2024 Oct 11;10(10):3650-3663. [Abstract]
- Br J Nutr. 2023 May 28;129(10):1657-1666. [Abstract]
- Cartilage. 2025 Nov 7:19476035251389178. [Abstract]
- STAR Protoc. 2024 Nov 2;5(4):103421. [Abstract]
- SSRN. 2025 Aug 13.
- Research Square Preprint. 2023 May 25.
- Evid Based Complement Alternat Med. 2022 Oct 10:2022:1897508. [Abstract]
- Research Square Print. 2022 Apr.
Customer Validation & Images
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WB
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RT-PCR
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Cell Migration/Invasion Assay
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WB
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Cell Imaging/Staining
Actividad biológica
pIC50: 7 (LXRα), 7.4 (LXRβ)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
<100 nM
Compound: 17, GSK-2033
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Inhibition of SREBP-1c expression in human HepG2 cells
Inhibition of SREBP-1c expression in human HepG2 cells
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[PMID: 20345102] |
| THP-1 | IC50 |
<100 nM
Compound: 17, GSK-2033
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Inhibition of ABCA1 expression in human THP1 cells
Inhibition of ABCA1 expression in human THP1 cells
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[PMID: 20345102] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1221277-90-2
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Appearance Solid
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Peso molecular 591.66
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Fòrmula C29H28F3NO5S2
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Color White to off-white
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (37)
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Journal Impact Factor
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Most Recent
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Immunity
25-Hydroxycholesterol regulates lysosome AMP kinase activation and metabolic reprogramming to educate immunosuppressive macrophages. [Abstract]2024 May 14;57(5):1087-1104.e7. PMID: 38640930 -
Mol Cell
mTOR inhibition reprograms cellular lipid homeostasis by inducing alternative lipid uptake and promoting cholesterol transport. [Abstract]2025 Sep 18;85(18):3486-3504.e7. PMID: 40972529 -
Sci Adv
ZMYND8 is a master regulator of 27-hydroxycholesterol that promotes tumorigenicity of breast cancer stem cells. [Abstract]2022 Jul 15;8(28):eabn5295. PMID: 35857506 -
Cell Death Differ
The lipogenic LXR-SREBF1 signaling pathway controls cancer cell DNA repair and apoptosis and is a vulnerable point of malignant tumors for cancer therapy. [Abstract]2020 Aug;27(8):2433-2450. PMID: 32144382 -
Environ Sci Technol
Impact of 1,2-Bis (2,4,6-Tribromophenoxy) Ethane on Liver Metabolism and Intestinal Health in Zebrafish: Role of the Liver X Receptor. [Abstract]2025 Apr 25. PMID: 40277015 -
Cancer Lett
Myeloid-derived suppressor cells deficient in cholesterol biosynthesis promote tumor immune evasion. [Abstract]2023 Jun 28:564:216208. PMID: 37150500 -
Phytomedicine
Qingre Sanjie Formula alleviates atherosclerosis by promoting LXR-α/ABCG5/G8-mediated reverse cholesterol transport and bile acid synthesis. [Abstract]2025 Jul:142:156691. PMID: 40286749 -
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Acta Pharmacol Sin
Celastrol induces lipophagy via the LXRα/ABCA1 pathway in clear cell renal cell carcinoma. [Abstract]2021 Sep;42(9):1472-1485. PMID: 33303989
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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J Transl Med
Mitochondrial dysfunction fuels drug resistance in adult T-cell acute lymphoblastic leukemia. [Abstract]2025 May 14;23(1):542. PMID: 40369632
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).
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Dev Cell
2026 Apr 29:S1534-5807(26)00150-4. PMID: 42061405 -
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Neural Regen Res
Thrombin increases the expression of cholesterol 25-hydroxylase in rat astrocytes after spinal cord injury. [Abstract]2023 Jun;18(6):1339-1346. PMID: 36453421
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.
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Clin Transl Med
TREM2 alleviates white matter injury after traumatic brain injury in mice might be mediated by regulation of DHCR24/LXR pathway in microglia. [Abstract]2024 Apr;14(4):e1665. PMID: 38649789 -
Cancer Immunol Res
Cholesterol Efflux Drives the Generation of Immunosuppressive Macrophages to Promote the Progression of Human Hepatocellular Carcinoma. [Abstract]2023 Oct 4;11(10):1400-1413. PMID: 37467346 -
Cell Rep
Probing the signaling requirements for naive human pluripotency by high-throughput chemical screening. [Abstract]2021 Jun 15;35(11):109233. PMID: 34133938 -
Brain Behav Immun
LXR-β regulates microglial efferocytosis and neuroinflammation in CPSP via STAT6 activation. [Abstract]2025 Aug 21:106089. PMID: 40848997 -
Brain Behav Immun
Activation of liver X receptors prevents emotional and cognitive dysfunction by suppressing microglial M1-polarization and restoring synaptic plasticity in the hippocampus of mice. [Abstract]2021 May:94:111-124. PMID: 33662504 -
Lipids Health Dis
Nitroxoline mitigates hepatic steatosis by enhancing cholesterol efflux and promoting bile acid synthesis through LRH-1 signaling. [Abstract]2025 Sep 29;24(1):296. PMID: 41023714 -
J Ethnopharmacol
Xiaoyan Lidan formula ameliorates cholecystitis by regulating cholesterol transportation and water permeability of the gall bladder through the activation of LXRβ. [Abstract]2026 Apr 6:360:121150. PMID: 41485629 -
J Ethnopharmacol
Radix Rehmanniae Praeparata extracts ameliorate hepatic ischemia-reperfusion injury by restoring lipid metabolism in hepatocytes. [Abstract]2024 Aug 20:335:118702. PMID: 39168395 -
J Ethnopharmacol
Qinghao-Biejia Herb Pair attenuates SLE atherosclerosis by regulating macrophage polarization via ABCA1/G1-mediated cholesterol efflux. [Abstract]2024 Jul 16:334:118545. PMID: 39002826 -
Ecotoxicol Environ Saf
Activation of LXRα attenuates 2-Ethylhexyl diphenyl phosphate (EHDPP) induced placental dysfunction. [Abstract]2023 Nov 1:266:115605. PMID: 37864966
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.
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Eur J Pharmacol
Cylindrin from Imperata cylindrica inhibits M2 macrophage formation and attenuates renal fibrosis by downregulating the LXR-α/PI3K/AKT pathway. [Abstract]2023 Jul 5:950:175771. PMID: 37146709 -
Int Immunopharmacol
Chalcone derivative 1m mitigates hepatic fibrosis and inflammation, enhances cholesterol efflux and reduces atherosclerosis. [Abstract]2025 Sep 23:162:115189. PMID: 40644861 -
Int J Mol Sci
TNFα Activates the Liver X Receptor Signaling Pathway and Promotes Cholesterol Efflux from Human Brain Pericytes Independently of ABCA1. [Abstract]2023 Mar 22;24(6):5992. PMID: 36983062 -
Biogerontology
Upregulation of LXRβ/ABCA1 pathway alleviates cochlear hair cell senescence of C57BL/6 J mice via reducing lipid droplet accumulation. [Abstract]2025 Jan 31;26(2):49. PMID: 39890652 -
J Cell Mol Med
The marine-derived furanone reduces intracellular lipid accumulation in vitro by targeting LXRα and PPARα. [Abstract]2020 Mar;24(6):3384-3398. PMID: 31981312 -
J Inflamm Res
Sirp-α Antibody Inhibits Renal Cell Carcinoma Progression via Akt1/Akt2 Modulation in Tumor-Associated Macrophages. [Abstract]2025 Oct 1:18:13575-13592. PMID: 41054626 -
ACS Infect Dis
Mycobacterium tuberculosis Suppresses Inflammatory Responses in Host through Its Cholesterol Metabolites. [Abstract]2024 Oct 11;10(10):3650-3663. PMID: 39360613 -
Br J Nutr
Oleic and palmitic acids induce hepatic angiopoietin-like 4 expression predominantly via PPAR-γ in Larimichthys crocea. [Abstract]2023 May 28;129(10):1657-1666. PMID: 34556193 -
Cartilage
Leucine Attenuates Osteoarthritis via mTORC1/LXRα-Mediated Macrophage Reprogramming and Rspo2/β-Catenin Axis Suppression. [Abstract]2025 Nov 7:19476035251389178. PMID: 41200799 -
STAR Protoc
2024 Nov 2;5(4):103421. PMID: 39488834 -
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Evid Based Complement Alternat Med
Ginsenosides Rg1 and CK Control Temozolomide Resistance in Glioblastoma Cells by Modulating Cholesterol Efflux and Lipid Raft Distribution. [Abstract]2022 Oct 10:2022:1897508. PMID: 36276866 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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
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.
| 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
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