Subtitle: Market Intelligence, Clinical Progress, and High-Purity Reagents for Transcriptional Regulation & Oncology Development.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for p300/EP300 drug discovery. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen (HAT Domain) | EP300 HAT Domain Recombinant Protein High purity (>95%), Endotoxin <1EU/ug. Sequence Verified. |
View EP300 Products |
| Antigen (Bromodomain) | EP300 Bromodomain Protein HEK293 Expressed (Native Folding). For selective inhibitor screening. |
View EP300 Products |
| Gene Delivery | EP300 Promise-ORF / Lentivirus Full-length ORF for stable cell line construction. |
View EP300 Products |
| Benchmark Ab | Anti-EP300 (ChIP-grade) Recombinant positive control for co-IP and ChIP assays. |
View EP300 Products |
| Validator | EP300 siRNA Set (3 unique sequences) For knockdown verification and specificity controls. |
View EP300 Products |
| Paralog Counter-screen | CREBBP (CBP) HAT Domain Protein Critical for paralog selectivity assays (75% homology). |
View CREBBP Products |
| Pathway Partner | BRD4 Recombinant Protein Bromodomain-containing partner for EP300 functional assays. |
View BRD4 Products |
| Related Target (Prostate Cancer) | AR (Androgen Receptor) Downstream pathway target in prostate cancer models. |
View AR Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| Paralog Selectivity (p300 vs CBP) | Human EP300 and CREBBP HAT domain proteins with >95% purity, Sequence Verified for homology region discrimination |
| Domain-Specific Inhibition | Modular domain constructs: HAT (aa 1195-1673), Bromodomain (aa 1095-1175), CH1/CH3/TAZ domains available |
| Enzymatic Activity Consistency | HEK293 Expressed proteins with native acetylation patterns; Endotoxin Controlled (<1 EU/μg) for cellular HAT assays |
| Structural Biology (Crystallography) | High Purity (>95% by SDS-PAGE and HPLC), Theoretical MW confirmed by Mass Spec; Tag-free options available |
| PROTAC Ternary Complex Validation | High-purity isolated domains (Bromodomain, HAT) tailored for SPR and TR-FRET |
| False Positives in Screening | Validated siRNA included for specificity checks and target validation |
Live p300/EP300 R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Global Clinical Landscape & Future Outlook
The race for p300/EP300-targeted therapeutics is intensifying, with major players shifting focus from pan-HAT inhibitors to highly selective p300/CBP paralog-selective small molecules and bifunctional degraders (PROTACs). As first-generation bromodomain and HAT inhibitors reach Phase I/II, the next wave of R&D is targeting domain-specific allosteric modulators that disrupt EP300's scaffolding functions independent of catalytic activity. Leveraging synthetic lethality between p300 and CBP, unique therapeutic windows are being explored in hematological malignancies and solid tumors.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Small Molecule (HAT Inhibitor) | CellCentric, AstraZeneca, AbbVie | Prostate Cancer, AML, Hematological Malignancies | Enzymatic HAT Assay / Selectivity Assay (Need active, purified HAT domain) |
| PROTAC Degrader | Arvinas, C4 Therapeutics, Dialectic Therapeutics | Solid Tumors, Castration-Resistant Prostate Cancer | Full-length Protein for ternary complex formation / SPR/TR-FRET |
| Bromodomain Inhibitor | Constellation (MorphoSys), GSK | Hematologic Malignancies | Bromodomain Binding Assay (Need properly folded BRD module) |
| Dual p300/CBP Inhibitor | Biogen, Roche | Rubinstein-Taybi Syndrome, Cancer | Paralog Selectivity Panel (Need both EP300 and CREBBP) |
| Combination Therapy (w/ AR inhibitors) | Various | Castration-Resistant Prostate Cancer | Pathway Validation (Need AR and p300 reagents) |
Key Structural Domains and Clinically Relevant Mutations
p300/EP300 (UniProt Q09472) contains several functional domains critical for its role as a transcriptional coactivator and histone acetyltransferase (HAT). The key domains include:
- KIX domain: Mediates interaction with transcription factors such as CREB.
- Bromodomain: Recognizes acetylated lysine residues on histones, facilitating chromatin binding.
- CBP/p300-type HAT domain: Catalyzes acetylation of histones and non-histone proteins (e.g., p53).
Clinically relevant mutations have been identified in EP300, including:
- dbSNP:rs2230111: A missense variant associated with altered activity.
- Breast cancer sample mutation (VAR_014428): Found in a breast cancer tumor sample, potentially driving oncogenesis.
- dbSNP:rs20551: Another common missense variant (Val/Leu) that may influence function.
These mutations underscore the importance of using sequence-verified reagents for studying EP300 biology and developing selective therapeutics.