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The dual specific threonine/tyrosine kinase, map kinase kinase (MEK), is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors.{6694,16830} CI-1040 is a benzhydroxamate compound that potently inhibits MEK in an in vitro mitogen-activated protein kinase cascade assay with an IC50 value of 2.3 nM (Kd = 74 nM when activated with adenosine triphosphate).{16877,15629} It can suppress phosphorylation of ERK in mouse colon 26 tumors with an IC50 value of 35 nM and demonstrates in vivo activity with oral administration in a mouse tumor model.{16877} The second-generation MEK inhibitor PD 0325901 (Item No. 13034) is a structural derivative of CI-1040 that was developed for improved solubility.{16877}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 10 mg, 25 mg, 5 mg, 50 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 212631-79-3 |
| Molecular formula | C17H14ClF2IN2O2 |
| Smiles | FC1=CC=C(C(NOCC2CC2)=O)C(NC3=C(Cl)C=C(I)C=C3)=C1F |
| Molecular weight | 478,7 |
| Custom code | 2922.19 |
| Formulation | A crystalline solid |
| Purity | ≥98% |
| 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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GPR17 is a G protein-coupled receptor that has been identified as a dualistic receptor recognizing signals from two unrelated chemical...
24(S),25-epoxy Cholesterol is an oxysterol and the most abundant oxysterol in mouse ventral midbrain.{43943} It activates liver X receptors (LXRs)...
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Protein phosphorylation is an important post-translational modification that serves many key functions to regulate a protein’s activity, localization, and protein-protein...
Adenosine Receptor A2A is a multi-pass membrane protein that is normally localized to the plasma membrane.{15465} This receptor is part...
GST-tag Polyclonal Antibody (FITC) is a probe for the immunochemical detection of GST tags on recombinant proteins. Recombinant proteins are...
(+)-D-threo-PDMP is a ceramide analog and is one of the four possible stereoisomers of PDMP (Item No. 62595).{11392} (+)-D-threo-PDMP is...
Nuclear factor erythroid 2-related factor 2 (Nrf2) is a basic leucine zipper transcription factor encoded by NFE2L2 in humans that...
This mixture contains primary prostaglandins produced from arachidonic acid and dihomo-?-linolenic acid. Contents: Prostaglandin E1, Prostaglandin E2, Prostaglandin F1?, 6-keto...
Proprotein convertase subtilisin kexin 9 (PCSK9) is a member of the subtilisin serine protease family with an important role in...
This rabbit anti-mouse IgA FITC is used as the ‘secondary antibody’ for immunostaining experiments where the primary antibody is mouse...
The Cayman COX Inhibitor Pack contains a combination of frequently used cyclooxygenase (COX) inhibitors. Each kit contains aspirin, the archetype...
CD34 is a transmembrane phosphoglycoprotein and sialomucin protein that is commonly used as a marker for hematopoietic progenitor cells.{59706,59704} It...
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