RGFP966 Suppresses Tumor Growth and Migration Through Inhibition of EGFR Expression in Hepatocellular Carcinoma Cells in vitro
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Updated: Dec 29, 2025
A Combined 3D Tissue Engineered In Vitro/In Silico Lung Tumor Model for Predicting Drug Effectiveness in Specific Mutational Backgrounds
Published on: April 6, 2016
Xinying Yu1, Fan Yang2, Hong Jiang3
1Second Pediatric Intensive Care Unit, Shengjing Hospital of China Medical University, Shenyang City, Liaoning Province, People's Republic of China.
Purpose:
Histone deacetylase 3 (HDAC3) has been suggested to play a role in hepatocellular carcinoma (HCC). In the present report, we aimed to identify the effects of RGFP966, a specific HDAC3 inhibitor, on the cell proliferation and migration of HCC cell lines.
Methods:
Human HCC cell lines, which were identified using short tandem repeat (STR) DNA profiling analysis, were used in this report. Cell proliferation assay was used to identify the growth viability of cells. Wound healing and transwell assay were used to identify the migration ability of cells. Further, a human phospho-receptor tyrosine kinases array kit was used to screen out RGFP966 effects on key receptor tyrosine kinases. Then, the mRNA expression was quantified by real-time PCR, and protein expression was identified by Western blot immunoassay.
Results:
We found that RGFP966 inhibited both proliferation and migration of HCC cells. Further, RGFP966 represses the expression and phosphorylation levels of epidermal growth factor receptor (EGFR) in HCC cells. Moreover, HDAC3 is involved in the inhibition of EGFR by RGFP966. Overall, we elucidated an inhibitive function of RGFP966 in HCC progression.
Conclusion:
RGFP966 inhibits EGFR signaling pathway and suppresses proliferation and migration of HCC cells.
Insights
RGFP966, an HDAC3 inhibitor, effectively suppresses hepatocellular carcinoma (HCC) cell proliferation and migration. This study reveals RGFP966
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Hepatocellular carcinoma (HCC) is a significant global health concern.
- Histone deacetylase 3 (HDAC3) is implicated in HCC development and progression.
- Targeting HDAC3 presents a potential therapeutic strategy for HCC.
Purpose of the Study:
- To investigate the effects of RGFP966, a specific HDAC3 inhibitor, on HCC cell lines.
- To determine the impact of RGFP966 on HCC cell proliferation and migration.
- To elucidate the molecular mechanisms underlying RGFP966's action in HCC.
Main Methods:
- Utilized human HCC cell lines identified via STR DNA profiling.
- Assessed cell proliferation using growth viability assays.
- Evaluated cell migration using wound healing and Transwell assays.
- Screened RGFP966 effects on receptor tyrosine kinases using a phospho-receptor tyrosine kinases array kit.
- Quantified mRNA and protein expression via real-time PCR and Western blot immunoassay, respectively.
Main Results:
- RGFP966 significantly inhibited proliferation and migration in HCC cells.
- RGFP966 repressed the expression and phosphorylation of epidermal growth factor receptor (EGFR).
- HDAC3 was identified as a key mediator in RGFP966's inhibition of EGFR.
- Demonstrated an overall inhibitory function of RGFP966 in HCC progression.
Conclusions:
- RGFP966 effectively inhibits EGFR signaling pathway in HCC.
- RGFP966 suppresses proliferation and migration of hepatocellular carcinoma cells.
- HDAC3 inhibition by RGFP966 offers a promising therapeutic avenue for HCC treatment.
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