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Protein Degraders

With the continuous advancement of antibody-drug conjugates (ADCs) toward precision and multifunctionality, protein degraders, as a new generation of payloads, are bringing revolutionary breakthroughs to targeted therapies. Unlike traditional small molecule inhibitors, protein degraders can induce complete degradation of pathological proteins via the ubiquitin-proteasome or lysosomal pathways, making them especially suitable for "undruggable" targets. BOC Sciences keeps pace with cutting-edge trends and leverages its strong expertise in small molecule synthesis, linker chemistry, and ADC conjugation technologies to build a one-stop platform for protein degrader development. We comprehensively support the full process from molecular design and structural optimization to DACs construction and functional validation, accelerating the development of next-generation ADCs.

What is a protein degrader?

Protein degraders are active molecules that specifically target and promote the degradation of proteins, serving as innovative cytotoxic or functional payloads in ADCs. They modulate key intracellular protein levels in tumor or pathological cells through mechanisms including the ubiquitin-proteasome system (UPS), lysosomal pathways, chaperone regulation, or targeted protein conformational interference. Common categories of protein degraders include PROTACs (Proteolysis Targeting Chimeras), molecular glues, small-molecule degraders, and other payloads that can be linked to ADCs.

Fig. 1. Protein degrader examples (BOC Sciences Authorized).

In ADC development, protein degraders are widely applied due to their high selectivity, controllability, and scalability, for instance, to degrade tumor-driving or drug-resistant proteins and enhance ADC antitumor activity and safety. Beyond ADCs, protein degraders are also employed in drug development, targeted cancer research, signal pathway analysis, target validation, and high-throughput screening platforms, providing core tool molecules for precision medicine, novel ADC platforms, and innovative anticancer drug design.

Key Challenges of Protein Degraders in ADC Research

Comprehensive  Product Line

Complex Structure of Degraders

Protein degraders typically have large, complex structures with multiple functional groups, which may affect conjugation efficiency and stability. BOC Sciences specializes in molecular modification and site selection to ensure efficient conjugation while preserving payload activity.

Competitive  Pricing

Poor Compound Stability of Degraders

Many degraders exhibit limited stability in vivo, impacting therapeutic performance. We provide linker optimization and encapsulation strategies to enhance metabolic stability and controlled release of the conjugates.

Flexible  Ordering Options

Immature Internalization and Release Mechanism

The intracellular delivery and release mechanisms of degrader-ADCs are not yet well established, making effect evaluation difficult. BOC Sciences offers comprehensive in vitro functional validation services from endocytosis and cleavage to target protein degradation.

Strict  Quality Control Testing

Limited Target Selection for Degradation

Current degrader-based ADCs focus on a limited range of targets and lack systematic development pathways and precedents. We assist clients in conducting target evaluation and early-stage mechanistic validation, supporting the transformation and druggability of new targets.

Protein Degrader-ADC Service Modules Offered by BOC Sciences

To promote innovative applications of protein degradation technologies in the ADC field, BOC Sciences has built a comprehensive service platform for protein degrader-ADCs, covering the entire process from degrader design, synthesis, and modification to conjugation strategy development and functional validation. We aim to integrate the concept of targeted protein degradation with efficient antibody delivery mechanisms, tailoring highly selective and stable next-generation degrader-ADC solutions to help overcome traditional payload limitations and expand therapeutic targets.

Degrader Molecular Design and Custom Synthesis

BOC Sciences possesses an experienced chemistry team capable of designing and synthesizing a wide range of protein degraders based on client-specific targets, including but not limited to PROTACs, molecular glues, and novel inducers such as LYTAC, AUTAC, MADTAC, and ATTEC. Our services include:

  • Target ligand screening and optimization
  • E3 ligase ligand selection (e.g., VHL, CRBN, MDM2, etc.)
  • Linker design and modification
  • Degrader stability and solubility enhancement

Degrader-Antibody Conjugation Strategy Development

To achieve efficient delivery, BOC Sciences provides personalized degrader conjugation technology services, including:

Degrader-Antibody Conjugates (DACs) Development

BOC Sciences now offers comprehensive DACs development services, coupling small molecule degraders as functional payloads to monoclonal antibodies for more precise delivery. The service includes:

  • Degrader screening and modification
  • Antibody selection and site-specific modification
  • DAC linker design
  • DAC stability and release testing
  • Target protein degradation verification

Degradation Activity Evaluation and Functional Validation

BOC Sciences supports in vitro functional evaluation of degrader-ADCs, including:

  • Target protein degradation assays (Western blot / ELISA)
  • Antigen binding validation
  • Cytotoxicity assessment (IC50, activity rescue assays)
  • Endocytosis and intracellular release efficiency testing
  • Ubiquitination level detection and mechanistic studies

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Comprehensive Strengths Empowering Next-Generation Degrader-ADCs

01

Innovative Cross-Platform Integration

BOC Sciences has deep expertise in both protein degradation technologies and ADC engineering. We integrate PROTACs, molecular glue, and monoclonal antibody conjugation to develop diverse degrader-ADC solutions, helping clients explore cutting-edge mechanisms and breakthrough targets.

02

Custom Degrader Molecular Design Services

We offer full-process custom services from target investigation, ligand screening to linker optimization. Combining structure-based design and pharmacophore modification, we create degraders with high selectivity, potent degradation activity, and favorable drug-like properties.

03

Diverse Conjugation Strategies and Linker Platforms

BOC Sciences has established a comprehensive conjugation chemistry platform, including amide bonds, click chemistry, ester bonds, and thiol-maleimide methods. We support both cleavable and non-cleavable linker development, enabling precise DAR control and site-specific conjugation to ensure conjugate stability and controlled release.

04

Comprehensive Analytical and Characterization Capabilities

Equipped with advanced analytical instruments and method platforms, we can comprehensively characterize DACs/ADCs in terms of purity, DAR, antibody integrity, and release efficiency. We also offer functional assessments such as target degradation, cytotoxicity, and ubiquitination analysis.

05

Scalable Process Development from mg to kg Levels

BOC Sciences possesses process development and scale-up capabilities under GMP conditions, enabling rapid scale-up of lab-grade degraders and conjugates to kilogram scale, ensuring stable supply and technical support for preclinical and clinical phases.

06

One-Stop ADC Drug Development Platform

Beyond protein degrader services, we also provide full-service ADC support, including antibody screening and engineering, humanization, linker design, conjugation process development, and pharmacology/toxicology evaluation—facilitating seamless transition of degrader-ADC projects from concept to IND filing.

Protein Degrader Development Service Workflow

Scheme Design and Contract Customization

Project Requirement Analysis and Target Evaluation

  • Understand the client's research goals and target characteristics
  • Analyze protein degradation feasibility and E3 ligase compatibility
  • Provide preliminary recommendations on target druggability and degradation strategies

Payload/Linker Synthesis

Degrader Molecular Design and Structural Optimization

  • Design core structures for PROTACs or molecular glues
  • Screen and synthesize target ligands and E3 ligase ligands
  • Develop various linker structures for SAR (Structure-Activity Relationship) analysis
  • Improve molecule permeability, water solubility, and stability

Scheme Design and Contract Customization

Degrader Synthesis and Purity Confirmation

  • Custom synthesis of small molecule degraders (mg–g scale)
  • Structural verification and purity analysis via HPLC, LC-MS, NMR, etc.
  • Provide chiral separation, chemical modification, and functional group introduction as needed

Analysis, Purification and Characterization

Degrader-Antibody Conjugates (DACs) Construction

  • Functionalize degraders (e.g., amine, carboxyl, azide) for conjugation
  • Select suitable antibodies and modify active sites (lysine, cysteine, or site-specific)
  • Design cleavable or non-cleavable linkers and perform conjugation reactions
  • Control the DAR and purify the final product

Result Delivery

Functional Validation and Mechanistic Evaluation

  • Evaluate target protein degradation activity (WB / ELISA)
  • Assess antibody binding and endocytosis capabilities
  • Conduct cytotoxicity and rescue assays
  • Investigate ubiquitination levels and degradation pathway mechanisms

cGMP Manufacturing and Filling

Process Scale-Up and Follow-Up Support

  • Provide pilot-scale synthesis of degraders or conjugates (g–kg scale)
  • Offer stability studies, impurity analysis, and storage condition optimization
  • Assist with preliminary in vivo pharmacokinetics and pharmacodynamics evaluation
  • Provide follow-up CMC development and IND support services if needed

Frequently Asked Questions

Frequently Asked Questions

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More About Protein Degraders

* Only for research. Not suitable for any diagnostic or therapeutic use.
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