To evaluate the effect of DC661 on PPT1 enzymatic activity and cell viability. Results showed that DC661 significantly reduced PPT1 enzymatic activity and led to loss of cell viability.
Induced M2 to M1 phenotype switching, evidenced by increased iNOS expression and decreased ARG1 and RETNLA/FIZZ1 expression.
JCI Insight. 2020 Sep 3;5(17):e133225
RAW 264.7 mouse macrophages
0.6 μM
24 h
Induced M2 to M1 phenotype switching, evidenced by increased iNOS expression and decreased ARG1 and RETNLA/FIZZ1 expression.
JCI Insight. 2020 Sep 3;5(17):e133225
Hep 1-6
3 µM
6 h
DC661 induced lysosomal membrane permeability, caused lysosomal deacidification, inhibited autophagy and enhanced sorafenib sensitivity in HCC cells.
Cancer Cell Int. 2022 Mar 11;22(1):115
Hep 3B
3 µM
6 h
DC661 induced lysosomal membrane permeability, caused lysosomal deacidification, inhibited autophagy and enhanced sorafenib sensitivity in HCC cells.
Cancer Cell Int. 2022 Mar 11;22(1):115
A375P cells
0-1000 nM
2 weeks
To assess the inhibitory effect of DC661 on long-term clonogenic growth, results showed that DC661 suppressed clonogenic growth more effectively than Lys05 or HCQ.
Cancer Discov. 2019 Feb;9(2):220-229
A375P cells
3 μM
6 h
To evaluate the effect of DC661 on lysosomal deacidification, results showed that DC661 caused significantly greater lysosomal deacidification compared to Lys05 or HCQ.
Cancer Discov. 2019 Feb;9(2):220-229
A375P cells
0-100 μM
1 h
To assess the inhibitory effect of DC661 on autophagic flux by microscopy, results showed that DC661 inhibited autophagic flux more effectively than Lys05 or HCQ.
Cancer Discov. 2019 Feb;9(2):220-229
A375P cells
0.1-10 μM
6 h
To evaluate the effect of DC661 on the accumulation of autophagic vesicle marker LC3BII, results showed that DC661 more significantly inhibited autophagic flux at lower concentrations compared to Lys05 or HCQ.
Cancer Discov. 2019 Feb;9(2):220-229
A375P
3 μM
24 h
Investigate the effect of DC661 on the proteome and lipidome of A375P cells, finding that DC661 significantly upregulates lipid metabolism enzymes and lipid species
Cancer Discov. 2023 Feb 6;13(2):454-473
DC661 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
Hepa1-6 subcutaneous HCC model
Intraperitoneal injection
3 mg/kg
Daily
DC661 enhanced the efficacy of anti-PD-1 antibody in HCC, significantly inhibited the growth of subcutaneous tumors, and increased tumor infiltration of MHC-II+ M1 macrophages and CD8+ T cells.
J Immunother Cancer. 2023 Jun;11(6):e006655
C57BL/6 mice
Hep 1-6-SR cell derived HCC tumor model
Intraperitoneal injection
3 mg/kg
Once daily for 21 days
DC661 combined with sorafenib significantly inhibited tumor growth and prolonged survival time in mice.
Cancer Cell Int. 2022 Mar 11;22(1):115
NSG mice
HT29 colorectal cancer xenograft model
Intraperitoneal injection
3 mg/kg
Daily
To evaluate the inhibitory effect of DC661 on tumor growth, results showed that DC661 significantly suppressed tumor growth without affecting mouse weight.
Cancer Discov. 2019 Feb;9(2):220-229
C57BL6 mice
B16-F10 melanoma model
Intraperitoneal injection
0.5 mg/kg
Once every two days
Investigate the effect of DC661 combined with eliglustat on B16-F10 tumor growth, finding that the combination significantly inhibited tumor growth
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