Drug intelligence / Profile preview

F0648-0589

Development stage
Preclinical
Lead developer
University of Texas MD Anderson Cancer Center
Modality
Small Molecules
01

Overview

F0648-0589 is a small molecule compound identified through in silico screening of approximately 4.9 million compounds as a potential inhibitor of Signal Transducer and Activator of Transcription 3 (Stat3) dimerization. It was one of 15 strong candidates selected for its ability to potentially block the protein-protein interactions required for Stat3 to form dimers and undergo nuclear translocalization. In experimental assays, F0648-0589 was one of four compounds that significantly inhibited the expression of IL-6 and RANKL, which are direct downstream targets of Stat3 signaling induced by IL-6. While it demonstrated potent in vitro activity in suppressing inflammatory cytokine expression, it was not the lead compound (F0648-0027) highlighted for in vivo efficacy in collagen-induced arthritis models in the primary study identifying these molecules.

02

Targets

STAT3 (Signal Transducer and Activator of Transcription 3)

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