Drug intelligence / Profile preview

SOX10 covalent inhibitor

Development stage
Preclinical
Lead developer
Massachusetts General Hospital
Modality
Small Molecules
01

Overview

SOX10 covalent inhibitor (specifically represented by the chemical probe SH-0029) is a first-in-class covalent small-molecule inhibitor and molecular glue targeting the lineage-restricted transcription factor SRY-box transcription factor 10 (SOX10). Developed by researchers at Massachusetts General Hospital and Harvard Medical School, the compound covalently binds to cysteine 71 (C71) of SOX10. This covalent engagement acts as a molecular glue that increases SOX10-SOX10 homodimerization, disrupting its DNA-binding and transcriptional activity in a dominant-negative manner. SH-0029 has demonstrated preclinical efficacy in inhibiting the proliferation of SOX10-dependent melanoma cells, including immunotherapy-resistant, acral, and uveal melanomas.

Other names
SOX10 covalent ligandSOX-10 covalent ligandSOX 10 covalent ligandSOX10 covalent molecular glueSOX-10 covalent molecular glueSOX 10 covalent molecular glue
02

Targets

SOX10 (SRY-box transcription factor 10)

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