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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

CAY10585

Cayman Chemical Item Number 10012682

Hypoxia Inducible Factor-1α Inhibitor (CAS 934593-90-5)

CAY10585 (CAS 934593-90-5)

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Description

Hypoxia inducible factor-1 (HIF-1) is a heterodimeric transcription factor composed of a HIF-1α subunit and HIF-1β subunit. Whereas the HIF-1β subunit is constitutively expressed, the HIF-1α subunit is regulated by cellular oxygen levels and therefore plays an important role in maintaining cellular oxygen homeostasis.1,2 Under normoxic conditions, HIF-1α is selectively hydroxylated on proline residues 402 and 577 and targeted for destruction by the ubiquitin-proteasome system. Under hypoxic conditions, HIF-1α accumulates and dimerizes with HIF-1β 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-1α accumulation and gene transcriptional activity.3 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-1α 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.3

1 Wang, G.L., Jiang, B., Rue, E.A., et al. Hypoxia-inducible factor 1 is a basic-helix-loop-helix-PAS heterodimer regulated by cellular O2 tension. Proc Natl Acad Sci USA 92 5510-5514 (1995).

2 Safran, M., and Kaelin, W.G. HIF hydroxylation and the mammalian oxygen-sensing pathway. J Clin Invest 111 779-783 (2003).

3 Lee, K., Lee, J.H., Boovanahalli, S.K., et al. (Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors. J Med Chem 50 1675-1684 (2007).

Synonyms
  • Hypoxia Inducible Factor-1α Inhibitor
Formal Name 4-​hydroxy-​3-​[[2-​(4-​tricyclo[3.3.1.13,​7]dec-​1-​ylphenoxy)acetyl]amino]-​benzoic acid,​ methyl ester
CAS Number 934593-90-5
Molecular Formula C26H29NO5
Formula Weight 435.5
Formulation A crystalline solid
Purity ≥97%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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COC(=O)​c1ccc(O)​c(NC(=O)​COc2ccc(cc2)​C2C3CC4CC(C3)​CC2C4)​c1

Background Reading

Wang, G.L., Jiang, B., Rue, E.A., et al. Hypoxia-inducible factor 1 is a basic-helix-loop-helix-PAS heterodimer regulated by cellular O2 tension. Proc Natl Acad Sci USA 92 5510-5514 (1995).

Safran, M., and Kaelin, W.G. HIF hydroxylation and the mammalian oxygen-sensing pathway. J Clin Invest 111 779-783 (2003).

Lee, K., Lee, J.H., Boovanahalli, S.K., et al. (Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors. J Med Chem 50 1675-1684 (2007).
Size Price Quantity Subtotal
1 mg $11.00 $0.00
5 mg $50.00 $0.00
10 mg $88.00 $0.00
25 mg $193.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-02-12. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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