WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H523111
CAS#: 1221277-90-2
Description: GSK-2033 is a potent cell-active LXR antagonist (pIC50 = 7.5). It enhances T-cell proliferation and blocks T 0901317-antiproliferative activity on T-cells and is cell permeable.
Hodoodo Cat#: H523111
Name: GSK-2033
CAS#: 1221277-90-2
Chemical Formula: C29H28F3NO5S2
Exact Mass: 591.14
Molecular Weight: 591.660
Elemental Analysis: C, 58.87; H, 4.77; F, 9.63; N, 2.37; O, 13.52; S, 10.84
Synonym: GSK-2033; GSK2033; GSK 2033.
IUPAC/Chemical Name: 2,4,6-Trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]benzenesulfonamide
InChi Key: PSOXOVKYGWBTPB-UHFFFAOYSA-N
InChi Code: InChI=1S/C29H28F3NO5S2/c1-19-14-20(2)28(21(3)15-19)40(36,37)33(18-25-12-13-27(38-25)29(30,31)32)17-22-8-10-23(11-9-22)24-6-5-7-26(16-24)39(4,34)35/h5-16H,17-18H2,1-4H3
SMILES Code: 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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively. |
| In vitro activity: | As shown in Fig. 1B, GSK2033 dose-dependently suppressed basal transcription in full-length LXRα or full-length LXRβ cotransfection assays with IC50s of 17 nM and 9 nM, respectively. GSK2033 also effectively suppressed the transcription of an ABCA1 driven luciferase reporter dose-dependently displaying IC50s of 52 nM for LXRα and 10 nM for LXRβ (Fig. 1C). Reference: Biochem Biophys Res Commun. 2016 Oct 21;479(3):424-428. https://pubmed.ncbi.nlm.nih.gov/27680310/ |
| In vivo activity: | TBD |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 5.0 | 8.45 | |
| DMSO | 17.5 | 29.51 |
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 |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Griffett K, Burris TP. 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. doi: 10.1016/j.bbrc.2016.09.036. Epub 2016 Sep 25. PMID: 27680310; PMCID: PMC5087326. |
| In vitro protocol: | 1. Griffett K, Burris TP. 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. doi: 10.1016/j.bbrc.2016.09.036. Epub 2016 Sep 25. PMID: 27680310; PMCID: PMC5087326. |
| In vivo protocol: | TBD |
1: Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA, Reid PR, Spearing PK, Stanley TB, Stewart EL, Willson TM. Discovery of tertiary sulfonamides as potent liver X receptor antagonists. J Med Chem. 2010 Apr 22;53(8):3412-6. doi: 10.1021/jm901797p. PubMed PMID: 20345102.
