Drug intelligence / Profile preview

YX862

Development stage
Preclinical
Lead developer
University of Florida
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01

Overview

YX862 is a selective histone deacetylase 8 (HDAC8) degrader developed by researchers at the University of Florida and Moffitt Cancer Center. It is designed to overcome resistance to BRAF and MEK inhibitors in BRAF V600E-mutated melanoma. HDAC8 overexpression has been linked to altered chromatin architecture and drug resistance in melanoma cells. YX862 functions by specifically degrading HDAC8, which leads to increased acetylation of SMC3, a component of the cohesin complex. This modification alters the three-dimensional structure of chromatin, potentially reversing the drug-resistant phenotype and inhibiting melanoma progression.

02

Targets

CRBN (Cereblon)HDAC8 (Histone Deacetylase 8)

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