Drug intelligence / Profile preview

bruceantinol

Development stage
Preclinical
Modality
Classical Binding Small Molecules → Small Molecules
Administration
Unknown
01

Overview

**Bruceantinol** is a natural quassinoid compound found in the fruits of *Brucea javanica*. It exhibits potent antitumor activity, acting primarily as an inhibitor of the STAT3 transcription factor. Bruceantinol directly binds STAT3 and prevents its activation and DNA binding at low nanomolar concentrations, resulting in the suppression of STAT3 target genes involved in anti-apoptosis and cell cycle regulation (such as MCL-1, PTTG1, survivin, and c-Myc). This mechanism leads to apoptosis, reduced proliferation and migration, and inhibited tumor growth in various preclinical cancer models, including colorectal cancer and osteosarcoma. Studies show bruceantinol is more effective in STAT3-dependent tumors and may also sensitize cancer cells to MEK inhibitors by overcoming resistance mechanisms. Beyond antineoplastic effects, bruceantinol displays antibacterial properties[1][3][5][7].

Other names
bruceantinol
02

Targets

STAT3 (Signal Transducer and Activator of Transcription 3)

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