GSK-J4 (hydrochloride)

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Cat No: 12073

Biochemicals - Small Molecule Inhibitors

The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-?-alanine, ethyl ester, monohydrochloride

Correlated keywords:

1373423-53-0 epigenetics demethylase histones JMJD3 cells differentiation developments inflammation cancers GSK-J1 pro-drug prodrugs H3 lysine 27 H3K27 H3K-27 GSKJ1 GSKs J1 GSKJ4 J4 inhibitors inhibits inhibitions macrophages reduce LPS induce induced proinflammatory inflammatory pro pro-inflammatory cytokines TNF.alpha. TNF-.alpha. TNF .alpha. TNF-alpha TNF-a TNF-? TNFalpha TNFa TNF? alpha ? HCl Structural Genomic Consortium SGC

Product Overview:
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.{21388} Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 µM).{21388}

Size	5 mg
Shipping	dry ice
CAS Number	1797983-09-5
Molecular Formula	C₂₄H₂₇N₅O₂ • HCl
SMILES	O=C(OCC)CCNC1=CC(N2CCC(C=CC=C3)=C3CC2)=NC(C4=CC=CC=N4)=N1.Cl
Molecular Weight	454
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.59
UNSPSC code	12352100

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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.