GSK126

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GSK126

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Cat No: 15415

Biochemicals - Small Molecule Inhibitors

The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} GSK126 is a selective, S-adenosyl-methionine-competitive s...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide

Correlated keywords:

histone H3-lysine H3 H3K27 methyltransferase EZH2 inhibitor inhibit HMT cancer GSK-126 S-adenosyl-methionine SAM S-adenosyl methionine S-adenosylmethionine trimethylation trimethylate PRC2 PRC-2 gene DLBCL xenografts chromatin research epigenetic modification KMT6

Product Overview:
The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} GSK126 is a selective, S-adenosyl-methionine-competitive small molecule inhibitor of EZH2 methyltransferase activity (Ki = 0.57 nM; IC50 = 9.9 nM versus that of EZH1: Ki = 89 nM; IC50 = 680 nM).{25456} It is more than 1,000-fold selective for EZH2 over other histone methyltranferases, including both SET-domain-containing and non-SET-domain-containing methyltransferases.{25456} At concentrations of 7-252 nM, it has been shown to inhibit global H3K27 trimethylation levels and to reactivate silenced PRC2 target genes.{25456} Furthermore, GSK126 can inhibit the proliferation of EZH2 mutant DLBCL cell lines (IC50 = 28-61 nM) as well as the growth of EZH2 mutant DLBCL xenografts in mice receiving a daily dose of 50 mg/kg.{25456}

Size	1 mg
Shipping	dry ice
CAS Number	1346574-57-9
Molecular Formula	C₃₁H₃₈N₆O₂
SMILES	CC1=CN([C@@H](C)CC)C2=CC(C(C=C3)=CN=C3N4CCNCC4)=CC(C(NCC5=C(C)C=C(C)NC5=O)=O)=C21
Molecular Weight	526,7
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.49
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.

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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.