Genz-123346 free base is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1 and IC50 for GM1 inhibition is 14 nM.
Genz-123346 free base 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Huh7 cells
5 µM
6 days
increased numbers of apoptotic and necrotic cells
Int J Mol Sci. 2024 Dec 31;26(1):304
Hepa 1-6 cells
5 µM
6 days
increased numbers of apoptotic and necrotic cells
Int J Mol Sci. 2024 Dec 31;26(1):304
Neonatal rat left ventricular myocytes (NRVMs)
100 μM
48 hours
Establish a cardiomyocyte hypertrophy model, results showed significant increase in mRNA expression of ANP, BNP, and β-MHC.
Front Pharmacol. 2024 Oct 1;15:1409625
HCT116 cells
5 µM
4 days
5 µM Genz significantly inhibited the cell cycle of HCT116 cells
Int J Mol Sci. 2021 Sep 29;22(19):10539
Lovo cells
1 µM and 5 µM
4 days
Genz treatment led to cell cycle arrest in G0/G1 phase and decreased cell numbers in S and G2/M phases in Lovo cells
Int J Mol Sci. 2021 Sep 29;22(19):10539
Mouse primary microglia
10 µM
72 h
Reduction in GM1 and GD1a levels and increased TNF mRNA expression upon LPS stimulation
J Neuroinflammation. 2022 Jan 6;19(1):9
BV2 cells
5-15 µM
72 h
Inhibition of UGCG activity, reduction in cellular GM1 and GD1a levels, and enhanced inflammatory response upon LPS stimulation
J Neuroinflammation. 2022 Jan 6;19(1):9
Dopaminergic neuronal cultures (DNCs)
5 μM
3–5 days
Reduced mTORC1 activity and increased TFEB expression
Front Neurosci. 2023 Jun 2;17:1152503
Neuronal Progenitor cells (NPCs)
5 μM
3–5 days
Inhibition of sphingolipid biosynthesis, reducing mTORC1 kinase activity and increasing TFEB levels
Front Neurosci. 2023 Jun 2;17:1152503
MDCK cells
10 μM
8 hours
To test the antiviral activity of GCS inhibitors against influenza virus A/PR/8/34 (H1N1), results showed that GZ-346 significantly inhibited viral RNA release
J Biol Chem. 2021 Jan-Jun;296:100470
Vero E6 cells
10 μM
24 hours
To test the antiviral activity of GCS inhibitors against SARS-CoV-2, results showed that GZ-346 significantly inhibited viral release
J Biol Chem. 2021 Jan-Jun;296:100470
Genz-123346 free base 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Jck mice (model of human nephronophthisis)
Oral
0.1% or 0.2% in feed
From 4 to 9 weeks of age
Genz-123346 treatment resulted in a dose-dependent reduction of renal GlcCer and GM3 levels that translated into effective inhibition of cystic disease
Nat Med. 2010 Jul;16(7):788-92
Mice
Experimental colon cancer model
Oral
0.225% Genz
10 weeks
Genz reduced the incidence of experimental colon cancer, particularly the growth of colorectal adenomas
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