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Chemical Structure : GNS561
CAS No.: 1914148-72-3
Catalog No.: PC-72561Not For Human Use, Lab Use Only.
GNS561 (Ezurpimtrostat, GNS-561) is a novel lysosomotropic agent and autophagy inhibitor that induces lysosomal cell death, targets palmitoyl-protein thioesterase 1 (PPT1).
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|---|---|---|---|
| 5 mg | $358 | In stock | |
| 10 mg | $558 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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GNS561 (Ezurpimtrostat, GNS-561) is a novel lysosomotropic agent and autophagy inhibitor that induces lysosomal cell death, targets palmitoyl-protein thioesterase 1 (PPT1).
GNS561 induced a dramatic increase of CSC death in both HCC and liver mCRC cell lines, displays antitumor properties in HCC in vivo models.
GNS561 activates the caspase-dependent apoptosis pathway, induces lysosomal membrane permeabilization and cathepsin-dependent cell death in HepG2 cells.
GNS561 showed potent antitumor activity ranging from 0.22 uM for the most sensitive cell line (LN-18, a glioblastoma cell line) to 7.27 uM for the least sensitive cell line (OVCAR3, ovarian cancer cell line).
GNS561 was at least 10-fold more effective than HCQ in tested cancer cell lines, also displayed activity in primary HCC patient-derived cells and was on average 3-fold more potent than sorafenib.
GNS561 exhibits potent antiviral activity against SARS-CoV-2 through autophagy inhibition.
| M.Wt | 422.99 | |
| Formula | C25H31ClN4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
2-Quinolinamine, N-[(4-chlorophenyl)methyl]-4-[4-[(1,1-dimethylethyl)amino]-1-piperidinyl]- |
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1. Sonia Brun, et al. Autophagy. 2021 Nov 5;1-17.
2. Bestion E, et al. Viruses. 2022 Jan 12;14(1):132. doi: 10.3390/v14010132.
3. Brun S, et al. J Cancer. 2021 Jul 13;12(18):5432-5438.
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