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GNS561

Chemical Structure : GNS561

CAS No.: 1914148-72-3

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GNS561 (GNS-561, Ezurpimtrostat)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 422.99
分子式 C25H31ClN4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-Quinolinamine, N-[(4-chlorophenyl)methyl]-4-[4-[(1,1-dimethylethyl)amino]-1-piperidinyl]-

参考文献

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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