WP1066

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WP1066

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Cat No: 14736

Biochemicals - Small Molecule Inhibitors

WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells when given at a concentration of 10 µM.{24389} It also induces apoptosi...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

3-(6-bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2E-propenamide

Correlated keywords:

inhibitors inhibits inhibitions cancers apoptosis neurosciences cardiovascular diseases immunology transcriptions factors WP-1066 WP1066 WPs 1066 cell-permeable cells permeable STAT3 STAT-3 STATs 3 three U87-MG U373-MG U87 U373 MGs U87MG U373MG malignant glioma apoptosis blood brain barrier blood-brain in vivo CD80 CD86 CDs 80 86 CD-80 CD-86 T T-cells seizures dephosphorylation nuclear exports phosphorylated induces orally bioavailables immune activations up-regulation up regulations proliferation induction effector T T-cells suppresses vascular smooth muscles injury mice seizures rats

Product Overview:
WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells when given at a concentration of 10 µM.{24389} It also induces apoptosis in U87-MG (IC50 = 5.6 µM) and U373-MG (IC50 = 3.7 µM) cells.{24389} WP1066 is orally bioavailable, crosses the blood-brain barrier, and demonstrates in vivo activity, including immune activation as indicated by the up-regulation of CD80 and CD86 and the induction of proliferation of effector T cells.{24390,24391} In addition to inducing apoptosis in cancer cells, WP1066 suppresses vascular smooth muscle cell proliferation after vascular injury in mice and prevents seizures following brain injury in rats.{24388,24392}

Size	1 mg
Shipping	dry ice
CAS Number	857064-38-1
Molecular Formula	C₁₇H₁₄BrN₃O
SMILES	BrC1=CC=CC(/C=C(C#N)/C(N[C@@H](C)C2=CC=CC=C2)=O)=N1
Molecular Weight	356,2
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2837.19
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.