EPZ6438

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EPZ6438

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Cat No: 16174

Biochemicals - Small Molecule Inhibitors

EPZ6438 is an orally bioavailable, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 2.5 nM), the enzymatic subunit of polycomb repressive complex 2.{28475} It displays a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative...

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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]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4'-(4-morpholinylmethyl)-[1,1'-biphenyl]-3-carboxamide

Correlated keywords:

inhibitor methyltranferase EZH2 H3K27 trimethylation cancer biochemical inhibit gene regulation modification EPZ-6438 orally bioavailable polycomb repressive complex PRC2 block wild-type lymphoma cell induce apoptosis differentiation SMARCB1-deleted maglinant rhabdoid tumor regression xenograft histone H3 lysine 27

Product Overview:
EPZ6438 is an orally bioavailable, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 2.5 nM), the enzymatic subunit of polycomb repressive complex 2.{28475} It displays a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other histone methyltransferases.{28475} EPZ6438 blocks histone H3 lysine 27 trimethylation in both wild-type and mutant lymphoma cells (IC50s range from 2-90 nM).{28476} EPZ6438 has been shown to induce apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor cells and to promote their regression in xenograft-bearing mice.{28475}

Size	1 mg
Shipping	dry ice
CAS Number	1403254-99-8
Molecular Formula	C₃₄H₄₄N₄O₄
SMILES	CC(C(N(C1CCOCC1)CC)=C2)=C(C(NCC3=C(C)C=C(C)NC3=O)=O)C=C2C4=CC=C(CN5CCOCC5)C=C4
Molecular Weight	572,7
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2922.19
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.