WDR5 (WD Repeat Domain 5) is a highly conserved scaffold protein essential for assembling diverse chromatin-associated complexes. It plays a pivotal role in the COMPASS-like family of histone methyltransferases (specifically interacting with MLL/KMT2 family members) and acts as a critical cofactor for the MYC oncogene. Consequently, WDR5 has emerged as a high-value therapeutic target in oncology, particularly for MLL-rearranged (MLL-r) leukemias, acute myeloid leukemia (AML), and MYC-driven solid tumors.
TarMart Solution Ecosystem & Related Targets
"Comprehensive reagent toolkit for WDR5 drug discovery. Select your modality below:"
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen | WDR5 Recombinant Protein (Wild Type & Mutants) High purity (>95%), Endotoxin controlled. Sequence Verified by Mass Spectrometry. |
View WDR5 Products |
| Gene Delivery | WDR5 Promise-ORF / Lentivirus Full-length ORF for stable cell lines, optimized for target validation and PROTAC degradation assays. |
View WDR5 Products |
| Benchmark Ab | Anti-WDR5 Recombinant Antibody High-affinity positive control for immunoprecipitation, Western blot, and chromatin assays. |
View WDR5 Products |
| Validator | WDR5 siRNA Set For target knockdown verification and target validation controls. |
View WDR5 Products |
| Related Target A | MLL1 (KMT2A) Core catalytic partner in the COMPASS complex; critical for validating WIN-site inhibitors. |
View MLL1 Products |
| Related Target B | MYC Oncogenic transcription factor; WDR5-MYC interaction is a key target for solid tumor therapeutics. |
View MYC Products |
| Related Target C | RBBP5 Core COMPASS subunit; essential for selectivity counter-screening against other WD40 repeat proteins. |
View RBBP5 Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| WIN-site PPI Disruption Validation | High-purity WDR5 (>95%) with conserved peptide-binding pocket conformation, sequence-verified by Mass Spectrometry. |
| Selectivity Counter-screening | Homologous WD40 domain proteins (e.g., RBBP5) strictly verified by SDS-PAGE and chromatography to eliminate off-target hits. |
| Resistance Mutation Profiling | Custom mutant proteins (e.g., F133A, D107A) available with theoretical MW verification for resistance-bypass screening. |
| Target Degradation (PROTAC) Assay | Lentiviruses expressing tag-fused WDR5 for high-throughput live-cell degradation and rescue assays. |
Live WDR5 R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Global Clinical Landscape & Future Outlook
The race for WDR5 therapeutics is intensifying, with major players shifting focus from traditional small-molecule inhibitors to targeted protein degraders (PROTACs). As first-generation therapies reach the clinic, the next wave of R&D is targeting the dual-site inhibition (disrupting both the MLL-binding WIN site and the MYC-binding WBM site) to overcome resistance and expand efficacy into solid tumors.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Small Molecule (WIN-site Inhibitors) | Boehringer Ingelheim, SGC | MLL-rearranged Leukemia, AML | Disruption assays (Need high-purity, structurally intact WDR5 recombinant protein) |
| PROTAC (Degraders) | Arvinas, University of Dundee | Hematological Malignancies, Solid Tumors | Degradation kinetics (Need WDR5 Lentivirus for stable cell line construction) |
| WBM-site Inhibitors (WDR5-MYC) | Vanderbilt University, Academic Spinoffs | MYC-driven Solid Tumors (Breast, Pancreatic) | Selectivity profiling (Need mutant proteins and MYC/WDR5 interaction assays) |