Epigenetic Regulation, Myeloid Malignancies, and High-Purity Reagents for Synthetic Lethality Development.
"Comprehensive reagent toolkit for ASXL1 drug discovery. Select your modality below:"
TarMart Solution Ecosystem & Related Targets
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen (Wild-Type) | ASXL1 ASXH Domain Recombinant Protein (covers HTH HARE-type and DEUBAD domains). High purity (>95%), Endotoxin <1EU/µg. Sequence Verified. Theoretical MW ~35 kDa. | View ASXL1 Products |
| Antigen (Mutant) | ASXL1 Truncated Mutant (G642fs*) Protein. CMML/AML-associated loss-of-function variant. Sequence Verified. | View ASXL1 Products |
| Gene Delivery | ASXL1 Promise-ORF / Lentivirus. Full-length ORF (1541 aa) for stable cell lines. CMV promoter, Puro selection. | View ASXL1 Products |
| Benchmark Ab | Anti-ASXL1 (Reference Clone). Recombinant rabbit monoclonal, validated for ChIP/WB. | View ASXL1 Products |
| Validator | ASXL1 siRNA Set (3 pre-designed). For knockdown verification. Sequence-verified specificity. | View ASXL1 Products |
| Binding Partner | BAP1 Recombinant Protein. Deubiquitinase partner for PR-DUB complex reconstitution. | View BAP1 Products |
| Pathway Related | EZH2 Recombinant Protein. PRC2 complex component, functional antagonist pathway. | View EZH2 Products |
| Disease Related | DNMT3A Mutant Proteins. Co-mutation target in myeloid malignancies. | View DNMT3A Products |
| Synthetic Lethal Partner | LSD1 Recombinant Protein. Epigenetic node frequently targeted in ASXL1-mutated AML. | View LSD1 Products |
| Paralog Selectivity | ASXL2 Recombinant Protein. Paralog for counter-screening. | View ASXL2 Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| PR-DUB Complex Reconstitution | ASXL1 ASXH Domain + BAP1 Catalytic Domain proteins available with >95% purity, endotoxin-controlled for enzymatic assays |
| Mutant vs Wild-Type Selectivity | Truncated mutant (G642fs*) and WT proteins strictly sequence-verified by mass spec for differential binding studies |
| Cellular Context Validation | Lentivirus particles for stable overexpression; ASXL1-specific siRNA for loss-of-function mimicry |
| ASXL Family Specificity | ASXL2 and ASXL3 ortholog proteins available for cross-reactivity screening (paralog selectivity assays) |
Live ASXL1 R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Global Clinical Landscape & Future Outlook
The ASXL1 therapeutic landscape is pivoting toward synthetic lethality and epigenetic combination strategies. As a recurrently mutated tumor suppressor in myeloproliferative neoplasms (present in ~40% of chronic myelomonocytic leukemia and ~20% of acute myeloid leukemia), ASXL1 loss-of-function creates specific dependencies on the residual PR-DUB complex and opposing PRC2 activity. Current R&D focuses not on direct ASXL1 restoration, but on exploiting the epigenetic vulnerability created by ASXL1 truncation—specifically targeting the hyperactive BAP1-dependent deubiquitination, the compensatory EZH2 methyltransferase activity, or downstream effectors like LSD1. Advanced modalities such as PROTACs are emerging to degrade the dominant-negative truncated proteins. The next wave of development emphasizes combination regimens pairing hypomethylating agents with novel chromatin modifiers.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Synthetic Lethality (Small Mol) | Preclinical Biotechs, Academic Labs | Myeloid Malignancies (ASXL1-mutant) | ASXL1-BAP1 Interaction Assay (Need purified ASXH domain + BAP1 complex) |
| EZH2 Inhibitor Combinations | Epizyme (Tazemetostat), Daiichi Sankyo | CMML, MDS | H3K27me3 / H2AK119Ub Cross-talk Assay (Need WT vs Mutant ASXL1 cellular models) |
| BAP1 Modulators | MorphoSys, Celgene (Bristol Myers) | Solid Tumors, Hematologic | Deubiquitination Activity Assay (Need high-purity recombinant proteins) |
| PROTAC Degraders | Undisclosed Biotech | ASXL1-Mutant Solid & Blood Cancers | Degradation Assays (Need Mutant Recombinant Proteins & Cell Lines) |
| Gene Therapy | Early Stage Academia | Rare Myeloid Disorders | Functional Validation (Need Lentivirus for stable expression rescue) |