GSK3987

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GSK3987

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Cat No: 30954

Biochemicals - Receptor Pharmacology

GSK3987 is a dual agonist of liver X receptor α (LXRα) and LXRβ.{57442} It recruits steroid receptor coactivator 1 (SRC-1) to LXRα and LXRβ in a ligand-sensing assay (LiSA; EC50s = 50 and 40 nM, respectively). GSK3987 is 50-fold selective for LXRα and...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

3-[(4-methoxyphenyl)amino]-4-phenyl-1-(phenylmethyl)-1H-pyrrole-2,5-dione

Correlated keywords:

GSK 3987 LXR SRC1 GSK 3? GSK3 ? ABCA THP1 IL6 interleukin SREBP1c Hep G2 HepG 2

Product Overview:
GSK3987 is a dual agonist of liver X receptor α (LXRα) and LXRβ.{57442} It recruits steroid receptor coactivator 1 (SRC-1) to LXRα and LXRβ in a ligand-sensing assay (LiSA; EC50s = 50 and 40 nM, respectively). GSK3987 is 50-fold selective for LXRα and LXRβ over a panel of nuclear receptors and GSK3β (IC50 = >5,000 nM) but does induce ABCA1 expression in a reporter assay using THP-1 cells (EC50 = 80 nM). It inhibits LPS-induced IL-6 secretion in THP-1 macrophages. GSK3987 increases the expression of the sterol regulatory element binding protein 1c (SREBP-1c) and induces triglyceride accumulation in HepG2 cells in a concentration-dependent manner.

Size	5 mg
Shipping	dry ice
CAS Number	264206-85-1
Molecular Formula	C₂₄H₂₀N₂O₃
SMILES	O=C(N1CC2=CC=CC=C2)C(C3=CC=CC=C3)=C(NC4=CC=C(OC)C=C4)C1=O
Molecular Weight	384,4
Formulation	A solid
Purity	≥98%
Custom Code	2922.49
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.