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Optimisation and mechanistic characterization of a selective benzoxazine-based MAP4K4 inhibitor in pancreatic cancer cells

Year: 2026
Type: article
Abstract: values of 4.41-4.65 μM and 4.03-5.12 μM, respectively. F389-0736 also inhibited clonogenic growth and induced sub-G1 accumulation with activation of apoptotic signalling. RNA sequencing identified 398 differentially expressed genes and revealed enrichment of inflammatory and stress response pathways, programmed cell death programs, oncogenic signalling perturbation, and metabolic reprogramming. These findings identify F389-0736 as a potent and selective benzoxazine-based MAP4K4 inhibitor and support its use as a chemical probe and lead scaffold for investigating MAP4K4-dependent signalling and therapeutic vulnerability in pancreatic cancer.
DOI: 10.1080/14756366.2026.2743434
Authors: Yi-Wen Wu, Chun-Lin Yang, Yu-Ting Fang-Chin, Yun-Hsuan Yeh, Bor-Jiun Chen, Tzu-Ying Sung, Jung-Chun Chu, Tony Eight Lin, Shih-Chung Yen, Jui-Hua Hsieh, Sing-Han Huang, Cheng-Ying Chu, Kai-Chien Yang, Kai-Cheng Hsu, Shiow-Lin Pan
Institutions: Taipei Medical University, Chinese University of Hong Kong, Chinese University of Hong Kong, Shenzhen, National Institutes of Health, National Institute of Environmental Health Sciences, National Taiwan University, Wan Fang Hospital
Language: English
Subfield: Oncology
Field: Medicine
Open Access status: gold
Estimated APC paid: $2,306
OpenAlex ID: W7222542563
FWCI:
Cites: 34
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