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hERG liability

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-175289

    Potassium Channel Sodium Channel Adrenergic Receptor Neurological Disease
    hERG-IN-3 is an orally active hERG blocker with an IC50 of 44.5 nM. hERG-IN-3 exhibits a Ki for β2-adrenergic receptor of 14 nM. hERG-IN-3 exhibits the skeletal muscle Nav1.4 and sodium channel-blocking activities (IC50 = 4.4 μM, 3-fold increasement than hNav1.5). hERG-IN-3 displays a potent antimyotonic activity in an animal model. hERG-IN-3 can be used for the study of Myotonia Congenita .
    hERG-IN-3
  • HY-175258

    Protein Arginine Deiminase Potassium Channel Neurological Disease Inflammation/Immunology Cancer
    PAD2/4-IN-1 (Compound 4f) is an orally active inhibitor of PAD2 and PAD4 with IC50 values of 23 nM and 10 nM, respectively. PAD2/4-IN-1 can inhibit protein citrullination in neutrophils and reduce hERG channel liabilities. PAD2/4-IN-1 can be used in the research of autoimmune diseases, neurological disorders, and cancers .
    PAD2/4-IN-1
  • HY-179622

    Methionine Adenosyltransferase (MAT) Cancer
    ZS34 is a potent, orally active, and selective MAT2A inhibitor with an IC50 of 13.7 nM, displaying minimal hERG and UGT1A1 liabilities. ZS34 selectively suppresses the growth of methylthioadenosine phosphorylase (MTAP)-deficient cancer cells by inhibiting SAM synthesis, reducing SDMA levels, and inducing DNA damage. ZS34 exhibits antitumor efficacy in a HCT116 MTAP -/- xenograft mouse model. ZS34 can be used for the research of MTAP-deficient cancer .
    ZS34

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