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The lysine methyltransferase EZH2 (KMT6), part of the polycomb repressive complex 2, catalyzes trimethylation of lysine 27 on histone H3 (H3K27me3) and is involved in proliferation and aggressive cell growth associated with neoplastic cells. CPI-169 is a selective EZH2 inhibitor with IC50 values of 0.24, 0.51, and 6.1 nM for wild-type EZH2, Y641N mutant EZH2, and wild-type EZH1, respectively.{29633} It decreases cellular levels of H3K27me3 (EC50 = 70 nM), triggering cell cycle arrest and ultimately resulting in apoptosis in a large panel of non-Hodgkin’s lymphoma (NHL) cell lines.{29633} With subcutaneous administration of 200 mg/kg/twice a day, CPI-169 was shown to inhibit tumor growth in a NHL xenograft model, reducing global H3K27me3.{29633} It has also been shown to synergize with the B-cell lymphoma 2 inhibitor, ABT-199 (Item No. 16233), to suppress the growth of NHL cell lines.{29633}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 1450655-76-1 |
| Molecular formula | C27H36N4O5S |
| Smiles | CC(NC1=O)=CC(OC)=C1CNC(C2=C(C)N(C(C)C3CCN(S(CC)(=O)=O)CC3)C4=C2C=CC=C4)=O |
| Molecular weight | 528,7 |
| Custom code | 2930.90 |
| Formulation | A crystalline solid |
| Purity | ≥98% |
| UNSPSC code | 12352100 |
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.
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