PFI-1

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PFI-1

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Cat No: 11155

Biochemicals - Small Molecule Inhibitors

Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of bromodomain-containing protein...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide

Correlated keywords:

BETs bromodomains inhibits inhibitors inhibition acetylateds lysines residues regulations nucleosomes chromatins structures genes expressions tandem bromodomain-containing proteins BRDs BRD2 BRD4 histones tails acetylations transcriptional targets promoters molecules therapeutics humans diseases inhibitory AlphaScreens assays PFI-1 PFI1 PFI 1 2 4 PF06405761 PFs 06405761 6405761 PF-06405761

Product Overview:
Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of bromodomain-containing protein (BRD) 2 and BRD4 bind acetylated histone tails, which couples histone acetylation marks to the transcriptional regulation of target promoters. Small molecule inhibitors of bromodomain interactions hold promise as useful therapeutics for human disease.{19044,19929,19950} PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. In an AlphaScreen assay it has been shown to inhibit BRD2 bromodomain 2 and BRD4 bromodomain 1 with IC50 values of 98 nM and 0.22 μM, respectively. See the Structural Genomics Consortium (SGC) website for more information.

Size	1 mg
Shipping	dry ice
CAS Number	1403764-72-6
Molecular Formula	C₁₆H₁₇N₃O₄S
SMILES	O=S(C1=C(OC)C=CC=C1)(NC2=CC=C(NC(N(C)C3)=O)C3=C2)=O
Molecular Weight	347,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2930.90
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.