Related Experiment Video

Updated: May 31, 2026

Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
09:20

Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS

Published on: August 10, 2017

Development of novel quinoline derivatives as selective HDAC6 inhibitors exhibiting multiple anticancer effects

Jie Peng1, Qianlong Zhao1, Changan Yu2

  • 1Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Jinan 250012, PR China.

Bioorganic Chemistry
|May 29, 2026
PubMed

Insights

A novel compound, P21, effectively inhibits histone deacetylase 6 (HDAC6), demonstrating significant anticancer effects. This potent HDAC6 inhibitor shows promise for further development as a new cancer therapeutic agent.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Histone deacetylase 6 (HDAC6) plays a crucial role in cellular functions.
  • HDAC6 overexpression is linked to cancer development and mortality.

Purpose of the Study:

  • To develop a potent and selective HDAC6 inhibitor.
  • To evaluate the anticancer potential of the optimized compound P21.

Main Methods:

  • Lead compound optimization (MPT0G211 to P21).
  • Western blot analysis for α-tubulin and histone H3 acetylation.
  • In vitro assays for anti-proliferative, anti-invasive, and anti-angiogenic activities, apoptosis, and cell cycle arrest.
  • In vivo efficacy study using a patient-derived xenograft (PDX) mouse model.

Main Results:

  • Compound P21 demonstrated improved potency and selectivity for HDAC6 inhibition.
  • P21 selectively increased α-tubulin acetylation without affecting histone H3.
  • P21 exhibited significant anti-proliferative, anti-invasive, and anti-angiogenic effects, induced apoptosis, and caused cell cycle arrest in vitro.
  • P21 showed notable anti-proliferative efficacy in vivo in a PDX mouse model.

Conclusions:

  • P21 is a potent and selective HDAC6 inhibitor with broad anticancer activities.
  • The findings support the further investigation of P21 as a potential anticancer therapeutic.
Keywords:
CancerHDAC6HDAC6 inhibitorHistone deacetylase

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