EN219

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EN219

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Cat No: 33957

Biochemicals - More Biochemicals

EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.{60543} It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50 = 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

1-[3,5-bis(4-bromophenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-chloro-ethanone

Correlated keywords:

EN-219 RNF-114 RNF114C8 p-21 TUBB-1 Hsp-60 D1 HspD-1 231-MFP BRD-4 HIST1-H3A

Product Overview:
EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.{60543} It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50 = 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 µM. EN219 (1 µM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP human breast cancer cells in a proteomic profiling assay. It has been linked to the bromodomain and extra terminal domain (BET) inhibitor ligand (+)-JQ1 for use as a proteolysis-targeting chimera (PROTAC) to degrade bromodomain-containing protein 4 (BRD4) in 231MFP cells.

Size	1 mg
Shipping	dry ice
CAS Number	380351-29-1
Molecular Formula	C₁₇H₁₃Br₂ClN₂O
SMILES	BrC(C=C1)=CC=C1C2N(C(CCl)=O)N=C(C3=CC=C(Br)C=C3)C2
Molecular Weight	456,6
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2933.69
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.

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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.