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Updated: May 5, 2026
Translationally-Relevant Tumor Resection Model for Murine Preclinical Models of Oral Squamous Cell Carcinoma
Published on: April 3, 2026
Antitumor effects of BI-D1870 on human oral squamous cell carcinoma
Chang-Fang Chiu1, Li-Yuan Bai, Naval Kapuriya
1Division of Hematology and Oncology, Department of Internal Medicine, China Medical University Hospital, Taichung, 40402, Taiwan.
Purpose:
Among the signaling pathways implicated in the tumorigenesis of oral squamous cell carcinoma (OSCC) is the extracellular signal-regulated kinase mitogen-activated protein kinase pathway, a downstream target of which is a family of serine/threonine kinases known as the 90 kDa ribosomal S6 kinases (RSKs). This study aims to investigate the role of BI-D1870, a specific inhibitor of p90 RSKs, in a panel of OSCC cell lines.
Methods:
The antitumor effects and mechanisms of BI-D1870 were assessed by MTT assays, flow cytometry, Western blotting, transfection, and confocal microscopy.
Results:
BI-D1870 exhibited a dose-responsive antiproliferative effect on OSCC cells with relative sparing of normal human oral keratinocytes. The compound inhibited the downstream RSK target YB-1 and caused apoptosis as evidenced by PARP cleavage, activation of the caspase cascade, and the presence of pyknotic nuclei in the 4,6-diamidino-2-phenylindole assay. In addition, BI-D1870 also induced G2/M arrest by modulating the expression of p21 and other cell cycle regulators. Other newly discovered anticancer attributes of BI-D1870 included the generation of reactive oxygen species and increases in endoplasmic reticulum stress and autophagy.
Conclusions:
Together, these results suggest the translational value of BI-D1870 in oral squamous cell carcinoma therapy.
Insights
BI-D1870, a specific inhibitor of 90 kDa ribosomal S6 kinases (RSKs), shows promising anticancer effects against oral squamous cell carcinoma (OSCC) by inducing apoptosis and cell cycle arrest. This suggests BI-D1870 has translational value for OSCC therapy.
Area of Science:
- Oncology
- Molecular Biology
- Cancer Signaling Pathways
Background:
- Oral squamous cell carcinoma (OSCC) tumorigenesis involves the extracellular signal-regulated kinase mitogen-activated protein kinase pathway.
- 90 kDa ribosomal S6 kinases (RSKs) are downstream targets within this pathway.
Purpose of the Study:
- To investigate the therapeutic potential of BI-D1870, a specific p90 RSK inhibitor, in OSCC.
- To elucidate the antitumor mechanisms of BI-D1870 in OSCC cell lines.
Main Methods:
- MTT assays for antiproliferative effects.
- Flow cytometry and Western blotting for apoptosis and cell cycle analysis.
- Confocal microscopy and transfection for mechanistic studies.
Main Results:
- BI-D1870 demonstrated dose-responsive antiproliferative effects on OSCC cells, sparing normal keratinocytes.
- The compound induced apoptosis via PARP cleavage and caspase activation, and G2/M arrest by modulating p21.
- BI-D1870 also triggered reactive oxygen species generation, endoplasmic reticulum stress, and autophagy.
Conclusions:
- BI-D1870 exhibits significant anticancer activity against OSCC.
- The findings support the translational potential of BI-D1870 for oral squamous cell carcinoma treatment.
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