Specification
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.
Synonyms
GSK-2033; GSK2033; GSK 2033
IUPAC Name
2,4,6-Trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]benzenesulfonamide
Canonical 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
InChI
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
InChI Key
PSOXOVKYGWBTPB-UHFFFAOYSA-N
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 58.87; H, 4.77; F, 9.63; N, 2.37; O, 13.52; S, 10.84
HS Tariff Code
2934.99.9001
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/
Shipping
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.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).