Cayman Ml-228;%; Sz- 10 Mg

Cayman Ml-228; N-([1,1-Biphenyl]-4-Ylmethyl)-6-Phenyl-3-(2-Pyridinyl)-1,2,4-Triazin-5-Amine; Purity- Greater Than Or Equal To 95%; Size- 10 Mg . 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. HIF-1α has emerged as an important drug target in breast and prostate cancer, cardiovascular disease and ischemia. ML-228 is an activator of the HIF signaling pathway, as demonstrated by HIF response element (HRE) reporter assay (EC50 = 1.2 uM), HIF-1α nuclear translocation assay (EC50 = 1.3 uM) and increased VEGF expression (EC50 = 1.6 uM). Its activity in the HRE assay is blocked by excess iron, suggesting that ML-228 can chelate iron.5 Molecular modeling indicates that ML-228 does not modulate HIF signaling by binding to prolyl hydroxyases. 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 - CAYM (Additional S&H Or Hazmat Fees May Apply)