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Structure–activity relationship

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8

Inhibitors & Agonists

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-124424

    Potassium Channel Others Neurological Disease
    VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC50=7.44 μM) and can be used for investigating Kir6.2/SUR1 expressed in the pancreas and brain. VU0071063 inhibits insulin secretion by inducing hyperpolarization of β-cell membrane potential. VU0071063 chemotype has a very steep structure-activity relationships .
    VU0071063
  • HY-155837

    Others Metabolic Disease
    hPL-IN-2 (compound 2u) is a potent, reversible, and non-competitive inhibitor of pancreatic lipase (IC50: 1.63 μM) and can be used in anti-obesity research .
    hPL-IN-2
  • HY-157928

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM) .
    Keap1-Nrf2-IN-18
  • HY-155316

    Others Others
    5-HT6R antagonist 2 (compound 29) is a 5-HT6 receptor antagonist .
    5-HT6R antagonist 2
  • HY-155836

    Others Metabolic Disease
    hPL-IN-1 (compound 2t) is a reversible inhibitor of pancreatic lipase (PL) (IC50=1.86 μM) for anti-obesity research .
    hPL-IN-1
  • HY-118851

    Others Others
    NSC-77053 is a potent BoNT/E inhibitor with an IC50 and a Ki of 2.4 μM and 1.29 μM, respectively .
    NSC-77053
  • HY-155138

    Glutaminase Metabolic Disease Cancer
    GLS1 Inhibitor-7 (compound 4d) is a GLS1 inhibitor (IC50=46.7 μM), with potential anti-cancer, anti-aging and anti-obesity properties .
    GLS1 Inhibitor-7
  • HY-158028

    Influenza Virus Infection
    PAN endonuclease-IN-2 (compound T-31) is a PAN endonuclease inhibitor (IC50: 0.15 μM) and antiviral agent with broad-spectrum anti- Influenza activity. PAN is the N-terminal PA subunit of the polymerase-RNA complex and the dependent endonuclease (CEN) active site. PAN initiates RNA replication by promoting cleavage of the RNA strand and allowing the polymerase to begin synthesizing new RNA molecules. PAN endonuclease-IN-2 targets both the influenza HA and RdRp complexes, thereby interfering with viral entry into host cells and viral replication .
    PAN endonuclease-IN-2

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