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Background <p>Methyl-CpG-binding domain protein 2 (MBD2) is a key epigenetic regulator implicated in tumorigenesis by repressing tumor suppressor genes by recognizing DNA methylation marks and recruiting specific histone-modifying enzymes and chromatin remodeling complexes. Although KCC-07 has been identified as a potent selective MBD2 inhibitor, its cytotoxic effects on various cancer cells remain largely unexplored. In the current study, we have examined the anti-proliferative and cytotoxic activities of KCC-07 on breast cancer (MCF-7), prostate cancer (PC-3), hepatocellular carcinoma (Huh-7), and osteosarcoma (U2-OS) cell lines, along with human skin fibroblasts (HFF-1) as a non-malignant control.</p> Methods and Results <p>Treatment of these cells with KCC-07 induced dose- and time-dependent cytotoxicity, notably reducing viability in Huh-7 and PC-3 cells. Flow cytometry analyses revealed that KCC-07 primarily triggered necrosis in Huh-7 and apoptosis in PC-3 cells. Furthermore, KCC-07 substantially downregulated MBD2-associated oncogenic targets such as <i>WNT1</i>, <i>CCND1</i>, and <i>ERK1/2</i> in Huh-7 and PC-3 cells without altering <i>MBD2</i> transcription.</p> Conclusion <p>These findings suggest that KCC-07 elicited a considerable cytotoxicity on cancer cells, likely modulating the expression of MBD2-related genes, highlighting its potential as a candidate for cancer therapy.</p> Graphical Abstract <p></p>

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A potent small-chemical MBD2 inhibitor, KCC-07, induces selective cytotoxicity in hepatocellular and prostate cancer cells

  • 期刊论文

  • 发表日期：

    2026年7月10日

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  • Kasım Kağan Koca,
  • Zeyneb Nur Akçay,
  • Gizem Kugu,
  • Fatma Özdemir,
  • Olcay Arman Gürer,
  • Merve Tuzlakoğlu Öztürk,
  • Uygar Halis Tazebay,
  • Ali Iftikhar,
  • Shafaat Ahmed Rabbani,
  • Zihni Onur Çalışkaner

摘要

Background

Methyl-CpG-binding domain protein 2 (MBD2) is a key epigenetic regulator implicated in tumorigenesis by repressing tumor suppressor genes by recognizing DNA methylation marks and recruiting specific histone-modifying enzymes and chromatin remodeling complexes. Although KCC-07 has been identified as a potent selective MBD2 inhibitor, its cytotoxic effects on various cancer cells remain largely unexplored. In the current study, we have examined the anti-proliferative and cytotoxic activities of KCC-07 on breast cancer (MCF-7), prostate cancer (PC-3), hepatocellular carcinoma (Huh-7), and osteosarcoma (U2-OS) cell lines, along with human skin fibroblasts (HFF-1) as a non-malignant control.

Methods and Results

Treatment of these cells with KCC-07 induced dose- and time-dependent cytotoxicity, notably reducing viability in Huh-7 and PC-3 cells. Flow cytometry analyses revealed that KCC-07 primarily triggered necrosis in Huh-7 and apoptosis in PC-3 cells. Furthermore, KCC-07 substantially downregulated MBD2-associated oncogenic targets such as WNT1, CCND1, and ERK1/2 in Huh-7 and PC-3 cells without altering MBD2 transcription.

Conclusion

These findings suggest that KCC-07 elicited a considerable cytotoxicity on cancer cells, likely modulating the expression of MBD2-related genes, highlighting its potential as a candidate for cancer therapy.

Graphical Abstract