A novel inhibitor of HIF-1a accumulation and gene transcriptional activity; inhibits HIF-1 transcriptional activity with IC50 values of 2.6 and 0.7 µM in human Hep3b and AGS cells

CAY10585 – 5 mg

Brand:
Cayman
CAS:
934593-90-5
Storage:
-20
UN-No:
Non-Hazardous - /

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.{11044,12428} 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.{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-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.{16441}  

 

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SKU: 10012682 - 5 mg Category:

Description

A novel inhibitor of HIF-1a accumulation and gene transcriptional activity; inhibits HIF-1 transcriptional activity with IC50 values of 2.6 and 0.7 µM in human Hep3b and AGS cells, respectively

Formal name: 4-hydroxy-3-[[2-(4-tricyclo[3.3.1.13,7]dec-1-ylphenoxy)acetyl]amino]-benzoic acid, methyl ester

Synonyms:  Hypoxia-Inducible Factor-1α Inhibitor

Molecular weight: 435.5

CAS: 934593-90-5

Purity: ≥97%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Prolyl Hydroxylation Enzymes||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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