PROTAC ERRα ligand 1

Background Introduction

PROTAC ERRα ligand 1 is a specialized small molecule designed to serve as the ligand component for targeting estrogen-related receptor alpha (ERRα) in PROTAC (Proteolysis Targeting Chimera) technology. ERRα, a nuclear hormone receptor, is implicated in various diseases, including cancer and metabolic disorders. Targeted degradation of ERRα via PROTACs can offer new therapeutic strategies for modulating its biological activity.

Mechanism

PROTAC ERRα ligand 1 functions by binding with high affinity and specificity to the estrogen-related receptor alpha (ERRα). When incorporated into a PROTAC construct, it facilitates the recruitment of ERRα to an E3 ubiquitin ligase complex (commonly via a covalently attached E3 ligase ligand), inducing the ubiquitination and subsequent proteasomal degradation of ERRα. This targeted protein degradation mechanism ensures selective removal of ERRα, offering advantages over traditional inhibitors by mediating sustained functional knockdown.

Applications

PROTAC ERRα ligand 1 is an essential building block for the design, synthesis, and optimization of ERRα-targeting PROTACs. Its main applications include:

• Development of small molecules for selective ERRα degradation in cancer and metabolic disease models
• Target validation studies to elucidate ERRα biology and function
• Structure-activity relationship (SAR) investigations in medicinal chemistry
• Custom synthesis of PROTACs for academic, pharmaceutical, and CRO research projects

By enabling efficient and selective degradation of ERRα, this ligand supports innovative targeted protein degradation approaches in drug discovery and functional genomics.

• High-purity compound verified by HPLC, NMR, and LC-MS
• Consistent batch-to-batch reproducibility with complete QC documentation
• Supplied with COA, MSDS, and analytical data for traceability
• Reliable global shipping with stability-guaranteed packaging
• Dedicated technical support and optional custom synthesis service
• Demonstrates strong binding affinity to CRBN, VHL, or other E3 ligases
• Enables stable E3 ligase recruitment for targeted protein degradation
• Selective ERRα targeting enables precise degradation of estrogen-related receptor alpha in PROTAC applications.
• Optimized ligand structure provides high binding affinity, enhancing the efficacy of targeted protein degradation strategies.