Custom PROTAC Synthesis Service

Targeted Protein Degradation (TPD) has emerged as a major breakthrough in modern drug discovery. Among TPD strategies, PROTACs (Proteolysis Targeting Chimeras) have gained considerable attention due to their ability to target previously “undruggable” proteins and overcome the limitations of traditional inhibitors. However, PROTAC synthesis and optimization often present multiple challenges, including the efficient construction of E3 ligase ligands and POI binders, rational linker design, purification and structural confirmation of complex molecules, and the validation of degradation efficacy both in vitro and in vivo. Without an integrated chemical synthesis and biological evaluation platform, such workflows are difficult to execute efficiently.

 

Built upon an integrated multi-omics platform and synergistic chem-biology capabilities, MtoZ Biolabs offers a comprehensive Custom PROTAC Synthesis Service, covering the entire workflow from E3 and POI ligand synthesis, linker design, to in vitro functional evaluation and in vivo pharmacological validation. We have supported numerous pharmaceutical and biotech companies worldwide, providing end-to-end solutions that accelerate the progression from concept to preclinical validation.

 

Services at MtoZ Biolabs

Our core services include:

1. Organic Synthesis-Support for E3 ligase ligands, POI binders, and various linker chemistries from milligram to gram scale.

2. High-Throughput Screening-Automated liquid handling and multi-mode plate readers enable rapid structure-activity relationship (SAR) exploration.

3. Advanced Analytical Tools-LC-MS/HRMS, HPLC, and NMR used for structure confirmation and purity assessment.

4. Cellular and Molecular Assays-Western blot, TR-FRET, NanoBRET, and multiple cell models support degradation validation.

5. ADME and Toxicology Support-Including solubility, plasma protein binding, cell permeability, and PK studies.

6. Functional Validation Support

• Target protein expression and degradation confirmation (Western blot, ELISA)
• Ternary complex formation assays (TR-FRET, AlphaLISA)
• Degradation kinetics analysis (DC50, Dmax)
• In vivo degradation evaluation using animal models

 

Analysis Workflow

 



 

Service Advantages

1. Integrated Chemical and Biological Platform

We streamline your project by consolidating synthesis, purification, and validation workflows within one platform. Equipped with LC-MS, NMR, HPLC, TR-FRET, and NanoBRET systems, we reduce coordination cost and accelerate timelines.

 

2. Diverse Ligand and Linker Resources

With extensive experience in synthesizing CRBN, VHL, MDM2, IAP ligands, and a modular linker library of various lengths and flexibilities, our Custom PROTAC Synthesis Service support rapid structural assembly and optimize ternary complex formation.

 

3. Automated High-Throughput Evaluation

Automated 96/384-well format screening enables parallel testing of degradation efficiency via TR-FRET, AlphaLISA, and NanoBRET. Selected hits can be further characterized using SPR or ITC.

 

4. Transparent Pricing and Comprehensive Deliverables

We operate on a flat-fee model with no hidden charges. Clients receive full analytical reports including HPLC, MS, NMR, and optional SPR, DLS, or ITC data, ready for internal review or publication.

 

5. Modular and Customizable Services

We provide modular services tailored to different stages of development. Whether you need linker-only synthesis, E3 ligand exploration, or full degradation analysis, we offer customized solutions. Complex targets and difficult-to-express proteins are also supported through method development.

 

Applications

1. PROTAC hit generation and SAR optimization

2. Exploration of previously undruggable targets

3. E3 ligase ligand development

4. Cancer, autoimmune, and inflammation research

5. Drug screening and target validation models

 

Sample Submission Suggestions

1. Target Information: Target name, UniProt ID, suggested E3 ligase, expression system or protein material

2. Lead Structure Information: POI binder or pharmacophore structure, desired linker type, known activity data

3. Sample Type and Quality: Chemical samples ≥3–10 mg, ≥95% purity; protein samples should include concentration, buffer, and storage info

4. Special Requirements: Animal testing, toxicity concerns, or biosafety issues should be clearly stated

 

For other sample types or project needs, please contact us for personalized guidance.

 

FAQ

Q1: Can you synthesize bifunctional or multi-target PROTACs?

A1: Yes, we support dual-ligand synthesis and ternary complex validation.

 

Q2: What’s the typical project turnaround time?

A2: Usually 4–8 weeks, depending on structural complexity and whether in vivo testing is included.

 

Deliverables

• Final PROTAC compound: Supplied as solid powder or DMSO solution, ready for biological assays and lead compound optimization.

• Product specification report: Includes batch information, formulation details, and storage conditions to support experimental reproducibility and regulatory documentation.

• Structural confirmation data: Verified by HPLC, MS, and NMR to ensure the accuracy, purity, and consistency of the compound structure.

• Degradation assay plots and raw data (if applicable): Generated from validated cellular models to support mechanism-of-action studies and compound screening.

• DC₅₀ / Dₘₐₓ analysis report (if applicable): Provides quantitative assessment of degradation potency, supporting informed decision-making in early-stage drug development.

 

With the growing importance of protein degradation in drug discovery, efficient synthesis and systematic evaluation of PROTACs has become essential. MtoZ Biolabs offers robust resources and expert-driven Custom PROTAC Synthesis Service to support your entire PROTAC development journey.

 

Contact us today for a customized proposal and quote. Let’s accelerate your PROTAC project together!