EZM2302

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EZM2302

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Cat No: 29954

Biochemicals - Small Molecule Inhibitors

EZM2302 is an inhibitor of protein arginine methyltransferase 4 (PRMT4; IC50 = 6 nM).{53436} It decreases asymmetric methylation of the PRMT4 substrate PABP1 (IC50 = 0.038 µM) and increases levels of demethylated SmB (EC50 = 0.018 µM) in RPMI-8226 mul...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

2-[2-[2-chloro-5-[(2R)-2-hydroxy-3-(methylamino)propoxy]phenyl]-6-(3,5-dimethyl-4-isoxazolyl)-5-methyl-4-pyrimidinyl]-2,7-diazaspiro[3.5]nonane-7-carboxylic acid, methyl ester

Correlated keywords:

GSK-3359088 EZM-2302 PRMT-4 PABP-1 methyl-transferase RPMI8226

Product Overview:
EZM2302 is an inhibitor of protein arginine methyltransferase 4 (PRMT4; IC50 = 6 nM).{53436} It decreases asymmetric methylation of the PRMT4 substrate PABP1 (IC50 = 0.038 µM) and increases levels of demethylated SmB (EC50 = 0.018 µM) in RPMI-8226 multiple myeloma cells. EZM2302 inhibits proliferation in a panel of 36 hematopoietic cancer cell lines, with IC50 values of less than 100 μM for nine of the 15 multiple myeloma cell lines included in the panel. It reduces tumor growth and decreases asymmetric PABP1 methylation in tumor tissue in an RPMI-8226 mouse xenograft model when administered at doses of 75, 150, and 300 mg/kg twice per day. Intrathecal injection of EZM2302 (10 µg) reduces acute mechanical allodynia and thermal hyperalgesia in a mouse model of neuropathic pain induced by chronic constriction injury (CCI).{53437}

Size	1 mg
Shipping	dry ice
CAS Number	1628830-21-6
Molecular Formula	C₂₉H₃₇ClN₆O₅
SMILES	ClC1=CC=C(OC[C@H](O)CNC)C=C1C2=NC(C3=C(C)ON=C3C)=C(C)C(N4CC5(CCN(C(OC)=O)CC5)C4)=N2
Molecular Weight	585,1
Formulation	A solid
Purity	≥98%
Custom Code	2933.39
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.