An activator of the HIF signaling pathway

ML-228 – 1 mg

Brand:
Cayman
CAS:
1357171-62-0
Storage:
-20
UN-No:
Non-Hazardous - /

The hypoxia-inducible factor (HIF) transcription factors are members of the basic-helix-loop-helix (bHLH) family of transcription factors and play important roles in maintaining cellular oxygen homeostasis.{11044,12428} HIF-1α has emerged as an important drug target in breast and prostate cancer, cardiovascular disease, and ischemia.{10724,11835} ML-228 is an activator of the HIF signaling pathway, as demonstrated by HIF response element (HRE) reporter assay (EC50 = 1.2 µM), HIF-1α nuclear translocation assay (EC50 = 1.3 µM), and increased VEGF expression (EC50 = 1.6 µM).{23099} Its activity in the HRE assay is blocked by excess iron, suggesting that ML-228 can chelate iron.{23099} Molecular modeling indicates that ML-228 does not modulate HIF signaling by binding to prolyl hydroxyases.{23099} ML-228 also significantly inhibits ligand binding to several channels, receptors, and transporters, including ERG potassium channel, 5-HT2B and A3 adenosine receptors, and dopamine transporter.{23099}  

 

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Description

An activator of the HIF signaling pathway, as demonstrated by HRE reporter assay (EC50 = 1.2 µM), HIF-1α nuclear translocation assay (EC50 = 1.3 µM), and increased VEGF expression (EC50 = 1.6 µM); activity is blocked by excess iron, suggesting that ML-228 can chelate iron

Formal name: N-([1,1′-biphenyl]-4-ylmethyl)-6-phenyl-3-(2-pyridinyl)-1,2,4-triazin-5-amine

Synonyms:  CID-46742353

Molecular weight: 415.5

CAS: 1357171-62-0

Purity: ≥95%

Formulation: A crystalline solid

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

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