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Methylstat (hydrate)

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    Methylstat (hydrate)
  • Methylstat (hydrate)
Cat No: 11091
Biochemicals - Small Molecule Inhibitors
Cayman
€55.00
Price is excluding VAT and does not include packaging neither shipping

Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability.{19980} The free acid of methylstat inhibits JMJD2A, JMJD2C, JMJD2E, PHF8, and JMJD3 with IC50 values of ap...

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Territorial Availability: Available through Bertin Pharma only in Europe
Synonyms:
  • 4-[hydroxy[4-[[[4-[[[(1-naphthalenylamino)carbonyl]oxy]methyl]phenyl]methyl]amino]butyl]amino]-4-oxo-2E-butenoic acid, methyl ester, monohydrate
Correlated keywords:
  • JMJD2A JMJD2C JMJD2E JMJD-2A JMJD-2C JMJD-2E JmjC PHF-8 pro-drug Jumonji C domain-containing histone demethylase methylation hyper-methylation 1310877-95-2
Product Overview:
Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability.{19980} The free acid of methylstat inhibits JMJD2A, JMJD2C, JMJD2E, PHF8, and JMJD3 with IC50 values of approximately 4.3, 3.4, 5.9, 10, and 43 µM, respectively, in an in vitro assay. Methylstat inhibits growth of the JMJD2C-sensitive esophageal cancer cell line KYSE150 with a GI50 of 5.1 µM, whereas the free acid of methylstat did not inhibit cell growth up to 100 µM. Methylstat induces histone hypermethylation at multiple sites in a concentration-dependent manner (EC50 for H3K4me3 and H3K9me3 = 10.3 and 8.6 µM in KYSE150 cells and 6.7 ad 6.3 µM in MCF-7 cells, respectively).
Size 1 mg
Shipping dry ice
Stability Store at -20 degrees; shelf life 730 days
Molecular Formula C28H31N3O6 • H2O
SMILES O=C(OCC1=CC=C(CNCCCCN(O)C(/C=C/C(OC)=O)=O)C=C1)NC2=CC=CC3=C2C=CC=C3.O
Molecular Weight 523,6
Formulation A crystalline solid
Purity ≥98%
Custom Code 2922.19
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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