An inhibitor of autophagy
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GNS561 (hydrochloride)

Item No. 45746

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(4-chlorophenyl)methyl]-4-[4-[(1,1-dimethylethyl)amino]-1-piperidinyl]-2-quinolinamine, monohydrochloride
CAS Number
1914148-73-4
Synonyms
  • Ezurpimtrostat
Molecular Formula
C25H31ClN4 • HCl
Formula Weight
459.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
CC(C)(NC(CC1)CCN1C2=C3C=CC=CC3=NC(NCC4=CC=C(Cl)C=C4)=C2)C.Cl
InChi Code
InChI=1S/C25H31ClN4.ClH/c1-25(2,3)29-20-12-14-30(15-13-20)23-16-24(28-22-7-5-4-6-21(22)23)27-17-18-8-10-19(26)11-9-18;/h4-11,16,20,29H,12-15,17H2,1-3H3,(H,27,28);1H
InChi Key
DLXMKLHCUTYCGO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $83

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    25 mg

    $145

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    50 mg

    $249

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    Product Description

    GNS561 is an inhibitor of autophagy.1 It inhibits palmitoyl-protein thioesterase 1 (PPT1) and autophagic flux, increases lysosomal zinc(II) levels, and induces apoptosis in HepG2 hepatocellular carcinoma (HCC) cells. GNS561 reduces viability in a panel of 17 human cancer cells (IC50s = 0.22-7.27 µM) and reduces alpha fetoprotein serum levels and tumor volume and weight in a patient-derived xenograft (PDX) mouse model of HCC. It also inhibits replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero E6 cells (EC50 = 0.04 µM) and reduces lung viral titers in a mouse model of SARS-CoV-2 infection.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brun, S., Bestion, E., Raymond, E., et al. GNS561, a clinical-stage PPT1 inhibitor, is efficient against hepatocellular carcinoma via modulation of lysosomal functions. Autophagy 18(3), 678-694 (2022).

    2. Bestion, E., Zandi, K., Belouzard, S., et al. GNS561 exhibits potent antiviral activity against SARS-CoV-2 through autophagy inhibition. Viruses 14(1), 132 (2022).