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Submit ReviewGSK 2033
Description: Potent LXR antagonist
Chemical Name: 2,4,6-Trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]benzenesulfonamide
Purity: ≥99% (HPLC)
Biological Activity for GSK 2033
GSK 2033 is a potent LXR antagonist (pIC50 = 7.5). Enhances T-cell proliferation and blocks T 0901317-antiproliferative activity on T-cells. Cell permeable.
Compound Libraries for GSK 2033
GSK 2033 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for GSK 2033
| M. Wt | 591.66 |
| Formula | C29H28F3NO5S |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1221277-90-2 |
| PubChem ID | 46203250 |
| InChI Key | PSOXOVKYGWBTPB-UHFFFAOYSA-N |
| Smiles | CC1=CC(C)=CC(C)=C1S(N(CC2=CC=C(C(F)(F)F)O2)CC(C=C3)=CC=C3C4=CC(S(C)(=O)=O)=CC=C4)(=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GSK 2033
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 11.83 | 20 |
Preparing Stock Solutions for GSK 2033
The following data is based on the product molecular weight 591.66. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 8.45 mL | 42.25 mL | 84.51 mL |
| 1 mM | 1.69 mL | 8.45 mL | 16.9 mL |
| 2 mM | 0.85 mL | 4.23 mL | 8.45 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.69 mL |
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Product Datasheets for GSK 2033
References for GSK 2033
References are publications that support the biological activity of the product.
Zuercher et al (2010) Discovery of tertiary sulfonamides as potent liver X receptor antagonists. J.Med.Chem. 53 3412 PMID: 20345102
Solt et al (2012) LXR-mediated inhibition of CD4+ T helper cells. PLoS ONE 7 e46615 PMID: 23029557
If you know of a relevant reference for GSK 2033, please let us know.
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Keywords: GSK 2033, GSK 2033 supplier, GSK2033, Potent, LXR, antagonists, liver, x, receptors, LXR-like, Receptors, 5694, Tocris Bioscience
7 Citations for GSK 2033
Citations are publications that use Tocris products. Selected citations for GSK 2033 include:
Hutchinson et al (2019) Phytosterols Inhibit Side-Chain Oxysterol Mediated Activation of LXR in Breast Cancer Cells. Int J Mol Sci 20 PMID: 31269628
Bruschi et al (2019) PNPLA3 I148M Variant Impairs Liver X Receptor Signaling and Cholesterol Homeostasis in Human Hepatic Stellate Cells. Hepatol Commun 3 1191 PMID: 31497741
Amaya et al (2023) Inhibition of LXR controls the polarization of human inflammatory macrophages through upregulation of MAFB. Cell Mol Life Sci 80 96 PMID: 36930354
Baek et al (2021) Liver x receptor alpha drives chemoresistance in response to side-chain hydroxycholesterols in triple negative breast cancer. Oncogene 40 2872-2883 PMID: 33742124
Keith S et al (2021) Listeria monocytogenes-infected human monocytic derived dendritic cells activate Vγ9Vδ2 T cells independently of HMBPP production. Sci Rep 11 16347 PMID: 34381163
Karen T et al (2020) The novel rexinoid MSU-42011 is effective for the treatment of preclinical Kras-driven lung cancer. Sci Rep 10 22244 PMID: 33335263
Bonney (2017) Differential Effects of Retinoic Acid Concentrations in Regulating Blood-Brain Barrier Properties. Eneuro 4 PMID: 28560318
Do you know of a great paper that uses GSK 2033 from Tocris? Please let us know.
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