Cayman mL-228

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.^1,2 HIF-1α has emerged as an important drug target in breast and prostate cancer, cardiovascular disease, and ischemia.^3,4 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).⁵ 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.⁵ mL-228 also significantly inhibits ligand binding to several channels, receptors, and transporters, including ERG potassium channel, 5-HT_2B and A₃ adenosine receptors, and dopamine transporter.⁵

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