Market Intelligence, Clinical Progress, and High-Purity Reagents for Epigenetic Targeting in Hematologic Malignancies and Solid Tumors.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for CREBBP (CBP, KAT3A) drug discovery. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen | CREBBP HAT Domain & Bromodomain Recombinant Proteins High purity (>95%), Endotoxin <1EU/ug. Sequence Verified. Theoretical MW confirmed by Mass Spec. HEK293 Expressed (Native Folding). Includes wild-type and key oncogenic mutant variants (e.g., HAT domain loss-of-function). |
View CREBBP Products |
| Gene Delivery | CREBBP Promise-ORF / Lentivirus Full-length ORF for stable cell lines (ChIP, HAT activity assays, PROTAC validation). |
View CREBBP Products |
| Benchmark Ab | Anti-CREBBP (Research Grade Monoclonal) Recombinant positive control for Western blot, IP, ChIP, and target engagement assays. |
View CREBBP Products |
| Validator | CREBBP siRNA Set For knockdown verification and specificity controls. |
View CREBBP Products |
| Paralog Control | EP300 (p300) HAT & Bromodomain Proteins Critical for selectivity assays vs. highly homologous paralog. |
View EP300 Products |
| Co-Target | BRD4 (Bromodomain Protein 4) For dual-targeting and selectivity profiling against BET family. |
View BRD4 Products |
| Pathway Partner | BCL6 Functional interactor in germinal center lymphomas; co-regulatory complex analysis. |
View BCL6 Products |
Note: Additional related targets such as CTNNB1 (β-catenin) for Wnt pathway disruption assays are available upon request.
Critical Assay Challenges & Technical Specifications
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| Paralog Selectivity (CREBBP vs EP300) | Purified HAT & Bromodomain proteins for both targets with >95% purity; Sequence Verified orthologs for orthogonal screening. |
| Domain-Specific Inhibitor Screening | Isolated domains available: HAT-only (aa 1193–1712), Bromodomain-only (aa 1086–1197), KIX domain, NCBD. No full-length protein contamination artifacts. |
| Intracellular Target Validation & PROTAC Degradation | High-titer Lentivirus for stable overexpression; validated siRNA; Endotoxin <5 EU/mL for sensitive cell lines. Supports ternary complex validation. |
| False Positives in Binding Assays | Negative control proteins (catalytically dead mutant e.g., R1441C) included; validated siRNA for specificity checks. |
| High-Throughput HAT Activity Assays | Sequence verified histone substrates (H3, H4) with confirmed acetylation sites. |
| Resistance Mutation Profiling | Disease-associated point mutants (e.g., HAT domain loss-of-function) available to model resistance and test next-generation inhibitors. |
Live CREBBP R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Global Clinical Landscape & Future Outlook
The race for CREBBP-targeted therapeutics is intensifying, with major players shifting focus from pan-epigenetic inhibitors to highly selective CBP/EP300 differentiation and novel modalities like PROTAC degraders. First-generation dual inhibitors (e.g., Foghorn's FHD-286) have advanced into Phase I/II for AML and follicular lymphoma, while next-generation programs target domain-specific inhibition (Bromodomain vs HAT) and bifunctional degraders to overcome paralog redundancy and resistance. Emerging molecular glue strategies aim to induce neomorphic interactions with transcription factors, opening new avenues for solid tumors and MYC-driven malignancies.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Dual CBP/EP300 Inhibitor | Foghorn (FHD-286), Daiichi Sankyo | AML, Follicular Lymphoma | Paralog Selectivity Panel (Need purified CREBBP & EP300 domains) |
| Domain-Specific Small Molecule | Novartis, CellCentric (CCS1477) | Prostate Cancer, DLBCL | Isolated Domain Binding (Need HAT-only vs BD-only proteins) |
| PROTAC Degrader | Academic/Preclinical Consortia | Solid Tumors (MYC-driven) | Cell-Based Validation (Need Lentivirus for stable cell lines, E3 ligase proteins) |
| Molecular Glue | Biotech Stealth Programs | Resistant Hematologic | Mutant Proteins (Need disease-associated point mutants for resistance profiling) |