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Hypoxia-inducible factor-1 (HIF-1) is a heterodimeric transcription factor composed of a HIF-1? subunit and HIF-1? subunit. Whereas the HIF-1? subunit is constitutively expressed, the HIF-1? subunit is regulated by cellular oxygen levels and therefore plays an important role in maintaining cellular oxygen homeostasis.{11044,12428} Under normoxic conditions, HIF-1? is selectively hydroxylated on proline residues 402 and 577 and targeted for destruction by the ubiquitin-proteasome system. Under hypoxic conditions, HIF-1? accumulates and dimerizes with HIF-1? to promote the transcription of a number of genes involved in angiogenesis, glycolysis, growth factor signaling, tumor invasion, and metastasis. CAY10585 is a novel small molecule inhibitor of HIF-1? accumulation and gene transcriptional activity.{16441} In a gene reporter assay using human Hep3B and AGS cell lines, CAY10585 prevented HIF-1 transcriptional activity with IC50 values of 2.6 and 0.7 µM, respectively. It blocks HIF-1? accumulation in Hep3B cells in a concentration and time-dependent manner, with complete inhibition at a concentration of 30 µM within 12 hours. CAY10585 also significantly suppresses transcription of the HIF-1 target genes VEGF and erythropoietin at 10 µM.{16441}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 25 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 934593-90-5 |
| Molecular formula | C26H29NO5 |
| Smiles | O=C(NC1=CC(C(OC)=O)=CC=C1O)COC2=CC=C(C3(C[C@@H](C4)C5)C[C@H]5CC4C3)C=C2 |
| Molecular weight | 435,5 |
| Custom code | 2916.31 |
| Formulation | A crystalline solid |
| Purity | ≥97% |
| 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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