@article{ART003203953},
author={Bong-Keun Jang and Ala Aiob and Woo Yeon Hwang and Dong Hoon Suh and Kidong Kim and Jae Hong No and Hye-Yeoun Kang and Hye Won Jeon and Yong Beom Kim},
title={BRD4 Inhibitor OPT-0010 Exerts Anticancer Effects Through Cell Cycle Arrest and Apoptotic Cell Death in Hepatic Carcinoma Cells},
journal={CELLMED},
issn={3022-6805},
year={2025},
volume={15},
number={6},
pages={7-19}
TY - JOUR
AU - Bong-Keun Jang
AU - Ala Aiob
AU - Woo Yeon Hwang
AU - Dong Hoon Suh
AU - Kidong Kim
AU - Jae Hong No
AU - Hye-Yeoun Kang
AU - Hye Won Jeon
AU - Yong Beom Kim
TI - BRD4 Inhibitor OPT-0010 Exerts Anticancer Effects Through Cell Cycle Arrest and Apoptotic Cell Death in Hepatic Carcinoma Cells
JO - CELLMED
PY - 2025
VL - 15
IS - 6
PB - Cellmed Orthocellular Medicine and Pharmaceutical Association
SP - 7
EP - 19
SN - 3022-6805
AB - Objective: Bromodomain-containing protein 4 (BRD4) is a critical transcriptional regulator of cell growth and differentiation. BRD4 inhibitors have the potential to curb cancer cell proliferation by downregulating the expression of associated genes. This study investigated the anticancer effects of a novel BRD4 inhibitor, OPT-0010, on human hepatic carcinoma cell lines.
Materials and Methods: Two hepatic carcinoma cell lines, SK-Hep1 and Huh-7, were subjected to 48-h OPT-0010 treatment. Cell viability and proliferation were evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and adenosine triphosphate assays, respectively. Flow cytometry was used to detect cell cycle arrest. Apoptotic cell death was evaluated using Annexin V and caspase 3 assays. BRD4 and apoptosis-related genes (e.g., BCL2 and BAX) and proteins (e.g., cleaved caspase-3, cleaved PARP, and BCL2) were evaluated using real-time polymerase chain reaction and western blotting, respectively. Additionally, a mouse xenograft model was used to analyze tumor growth, weight, and messenger RNA (mRNA) levels.
Results: OPT-0010 significantly decreased cell viability and proliferation, inducing cell cycle arrest and apoptotic cell death in both SK-Hep1 and Huh-7 cell lines. OPT-0010 showed substantial anti-tumor efficacy in a mouse xenograft model, affecting tumor growth and the expression of BRD4 and apoptosis-related proteins. Furthermore, in synergy with sorafenib, OPT-0010 exhibited an enhanced effect, increasing apoptotic cell death, and effectively suppressing tumor growth in vitro and in vivo.
Conclusion: This study provided comprehensive insights into the mechanisms and therapeutic effects of OPT-0010 on human hepatic carcinoma cell lines and in vivo mouse xenograft models. These results suggest that OPT-0010 is a promising therapeutic agent for treating human hepatocellular carcinoma.
KW - BRD4 inhibitor;OPT-0010;hepatic carcinoma;cell viability;apoptosis;tumor growth;synergistic effect
DO -
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ER -
Bong-Keun Jang, Ala Aiob, Woo Yeon Hwang, Dong Hoon Suh, Kidong Kim, Jae Hong No, Hye-Yeoun Kang, Hye Won Jeon and Yong Beom Kim. (2025). BRD4 Inhibitor OPT-0010 Exerts Anticancer Effects Through Cell Cycle Arrest and Apoptotic Cell Death in Hepatic Carcinoma Cells. CELLMED, 15(6), 7-19.
Bong-Keun Jang, Ala Aiob, Woo Yeon Hwang, Dong Hoon Suh, Kidong Kim, Jae Hong No, Hye-Yeoun Kang, Hye Won Jeon and Yong Beom Kim. 2025, "BRD4 Inhibitor OPT-0010 Exerts Anticancer Effects Through Cell Cycle Arrest and Apoptotic Cell Death in Hepatic Carcinoma Cells", CELLMED, vol.15, no.6 pp.7-19.
Bong-Keun Jang, Ala Aiob, Woo Yeon Hwang, Dong Hoon Suh, Kidong Kim, Jae Hong No, Hye-Yeoun Kang, Hye Won Jeon, Yong Beom Kim "BRD4 Inhibitor OPT-0010 Exerts Anticancer Effects Through Cell Cycle Arrest and Apoptotic Cell Death in Hepatic Carcinoma Cells" CELLMED 15.6 pp.7-19 (2025) : 7.
Bong-Keun Jang, Ala Aiob, Woo Yeon Hwang, Dong Hoon Suh, Kidong Kim, Jae Hong No, Hye-Yeoun Kang, Hye Won Jeon, Yong Beom Kim. BRD4 Inhibitor OPT-0010 Exerts Anticancer Effects Through Cell Cycle Arrest and Apoptotic Cell Death in Hepatic Carcinoma Cells. 2025; 15(6), 7-19.
Bong-Keun Jang, Ala Aiob, Woo Yeon Hwang, Dong Hoon Suh, Kidong Kim, Jae Hong No, Hye-Yeoun Kang, Hye Won Jeon and Yong Beom Kim. "BRD4 Inhibitor OPT-0010 Exerts Anticancer Effects Through Cell Cycle Arrest and Apoptotic Cell Death in Hepatic Carcinoma Cells" CELLMED 15, no.6 (2025) : 7-19.
Bong-Keun Jang; Ala Aiob; Woo Yeon Hwang; Dong Hoon Suh; Kidong Kim; Jae Hong No; Hye-Yeoun Kang; Hye Won Jeon; Yong Beom Kim. BRD4 Inhibitor OPT-0010 Exerts Anticancer Effects Through Cell Cycle Arrest and Apoptotic Cell Death in Hepatic Carcinoma Cells. CELLMED, 15(6), 7-19.
Bong-Keun Jang; Ala Aiob; Woo Yeon Hwang; Dong Hoon Suh; Kidong Kim; Jae Hong No; Hye-Yeoun Kang; Hye Won Jeon; Yong Beom Kim. BRD4 Inhibitor OPT-0010 Exerts Anticancer Effects Through Cell Cycle Arrest and Apoptotic Cell Death in Hepatic Carcinoma Cells. CELLMED. 2025; 15(6) 7-19.
Bong-Keun Jang, Ala Aiob, Woo Yeon Hwang, Dong Hoon Suh, Kidong Kim, Jae Hong No, Hye-Yeoun Kang, Hye Won Jeon, Yong Beom Kim. BRD4 Inhibitor OPT-0010 Exerts Anticancer Effects Through Cell Cycle Arrest and Apoptotic Cell Death in Hepatic Carcinoma Cells. 2025; 15(6), 7-19.
Bong-Keun Jang, Ala Aiob, Woo Yeon Hwang, Dong Hoon Suh, Kidong Kim, Jae Hong No, Hye-Yeoun Kang, Hye Won Jeon and Yong Beom Kim. "BRD4 Inhibitor OPT-0010 Exerts Anticancer Effects Through Cell Cycle Arrest and Apoptotic Cell Death in Hepatic Carcinoma Cells" CELLMED 15, no.6 (2025) : 7-19.
