Market Intelligence, Clinical Progress, and High-Purity Reagents for Oncology, Epigenetic, and CNS Drug Development.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for KDM1A (LSD1) drug discovery. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen / Target Enzyme | KDM1A (LSD1) Recombinant Protein (Full Length & Catalytic Domain). High purity (>95%), Endotoxin <1 EU/μg. Sequence Verified. Theoretical MW confirmed. Available in WT, catalytic-dead (K661A), and mutant variants for resistance studies. | View KDM1A Products |
| Gene Delivery | KDM1A Promise-ORF / Lentivirus. Full-length ORF for stable cell line generation. HEK293T expressed. | View KDM1A Products |
| Benchmark Ab | Anti-KDM1A (Research Grade). Recombinant monoclonal for Western/IP/ChIP detection. Sequence Verified positive control. | View KDM1A Products |
| Validator | KDM1A siRNA Set (3 unique targets). For knockdown verification and specificity controls. | View KDM1A Products |
| Related Target A | KDM1B (LSD2). Synergistic H3K4me2 demethylase; paralogue selectivity screening. | View KDM1B Products |
| Related Target B | MAOA. Primary off-target liability; flavin oxidase homology requires counter-screening. | View MAOA Products |
| Related Target C | RCOR1 (CoREST). Essential corepressor complex partner for LSD1 functional assays and PPI studies. | View RCOR1 Products |
| Related Target D | HDAC1. CoREST complex partner; rational combination target with KDM1A inhibitors. | View HDAC1 Products |
| Related Target E | KDM5C (SMCX). JmjC demethylase – compensatory mechanism & combination studies. | View KDM5C Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| MAO-A/B selectivity counter-screening | Homolog panel proteins (KDM1A, MAOA, MAOB) strictly verified by mass spec; >95% purity for exclusion of off-target flavin oxidase activity. |
| Acquired drug resistance profiling | KDM1A mutant recombinant proteins (e.g., K661A, gatekeeper mutants) available for resistance mechanism studies and next-generation screening. |
| PROTAC degradation monitoring | Sequence Verified ORFs and High-Purity Proteins for quantitative western and mass spec standards. siRNA for knockdown correlation. |
| Complex formation & PPI (LSD1-CoREST) | High-purity recombinant targets for strict stoichiometric binding analyses; Co-complex with RCOR1 available for physiologically relevant conformation. |
| Biochemical assay drift & false positives | Endotoxin-controlled (<1 EU/μg), high-purity WT protein with Theoretical MW for HTRF/AlphaLISA/SPR. |
| Species translation (Mouse/Cyno models) | Mouse and Cynomolgus ortholog proteins with sequence-verified fidelity for preclinical PK/PD studies. |
Live KDM1A R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Global Clinical Landscape & Future Outlook
The KDM1A/LSD1 inhibitor landscape is transitioning from non-selective MAOI scaffolds to highly selective mechanism-driven inhibitors, reversible modalities, and targeted degraders. First-generation irreversible inhibitors (iadademstat, bomedemstat) have established proof-of-concept in hematologic malignancies (AML, myelofibrosis) and SCLC, but MAO cross-reactivity and hematological toxicities (thrombocytopenia) limit their therapeutic index. This has accelerated investment in reversible inhibitors, allosteric modulators, PROTACs, and CNS-penetrant strategies. The next wave of R&D targets the scaffolding function of LSD1, disrupting protein-protein interactions (e.g., with GFI1/CoREST) to overcome resistance and broaden indications. Combination therapies with HDAC inhibitors, DNMT inhibitors, and PD-(L)1 antibodies are emerging as standard approaches in AML, MDS, and solid tumors. For neurodegenerative applications (Alzheimer's, Huntington's), blood-brain barrier-penetrant modalities are under early clinical investigation.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Irreversible Small Molecule Inhibitor | Oryzon (iadademstat), Imago/BMS (bomedemstat), Incyte | AML, Myelofibrosis, SCLC | Biochemical screening: need high-purity enzyme + homolog panel (KDM1A, MAO) for selectivity. |
| Reversible Small Molecule Inhibitor | Salarius (seclidemstat), Celgene/BMS, academic | Ewing Sarcoma, Solid Tumors | Binding kinetics/SPR: need strictly controlled theoretical MW protein for reliable Kd measurements. |
| PROTAC / Degrader | Preclinical / Emerging Biotech | Refractory Solid Tumors, Prostate Cancer | Cellular degradation assay: need high-quality antibodies and siRNA for DC50/Dmax quantification. |
| PPI / Scaffolding Disruptor | Academic / Early Biotech | SCLC, AML | Scaffolding validation: need RCOR1/CoREST accessory proteins for ternary complex formation assays. |
| CNS-Penetrant Inhibitor | Oryzon (ORY-2001) | Alzheimer's Disease | Blood-brain barrier models: need lentiviral ORF for iPSC-derived neuronal target engagement studies. |
| Combination (Hypomethylating) | Multiple Academia | MDS/AML Resistance | Synergy assays with AZA: need mutant proteins to study resistance mechanisms. |
Key Considerations for Best-in-Class Drug Differentiation
To succeed in the competitive KDM1A landscape, next-generation molecules must demonstrate:
- Affinity & Kinetics: High binding affinity (low nM Kd) and suitable target residence time (SPR-validated).
- Mechanism Clarity: Differentiate between catalytic FAD-pocket inhibition, allosteric disruption of protein-protein interactions, or targeted degradation (PROTAC).
- Safety Profile: Avoid thrombocytopenia by sparing normal hematopoietic stem cell lineages; minimize MAO-A/B off-target activity.
- Resilience to Resistance: Preemptively profile against identified resistance mutations (e.g., K661A, FAD-binding site changes).