SGC 0946
Potent and Selective DOT1L Histone Methyltransferase Inhibitor
SGC 0946
CAT#: 0957-S7079-10mg
Size: 10 mg
CAS Number: 1561178-17-3
Target: Histone Methyltransferase (DOT1L)
Research Area: Epigenetics
Dry Ice: Yes
Hazardous: No
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
Product Description
SGC 0946 is a potent and selective small-molecule inhibitor of DOT1L (Disruptor of Telomeric Silencing 1-Like), a histone methyltransferase involved in epigenetic regulation of gene expression.
DOT1L catalyzes the methylation of lysine 79 on histone H3 (H3K79), a modification associated with chromatin organization and transcriptional regulation. By inhibiting DOT1L activity, SGC 0946 provides a research tool for investigating histone methylation and epigenetic mechanisms.
SGC 0946 exhibits an IC50 value of 0.3 nM in a cell-free assay and demonstrates selectivity over a panel of 12 protein methyltransferases (PMTs) and DNMT1.
Key Features
- Potent and selective DOT1L methyltransferase inhibitor
- IC50: 0.3 nM in a cell-free assay
- Target: DOT1L histone methyltransferase
- Designed for epigenetics research
- Investigates H3K79 histone methylation
- Shows selectivity against a panel of 12 PMTs and DNMT1
Mechanism of Action
DOT1L is responsible for catalyzing histone H3 lysine 79 methylation (H3K79me), a key epigenetic modification. SGC 0946 inhibits DOT1L enzymatic activity, allowing researchers to investigate the biological consequences of reduced H3K79 methylation.
This inhibition provides a useful approach for studying chromatin-associated processes, transcriptional regulation and epigenetic signaling pathways.
Research Applications
- Epigenetic regulation and chromatin biology
- Histone H3K79 methylation studies
- DOT1L enzyme activity investigations
- Histone methyltransferase inhibitor screening
- Gene expression and transcriptional regulation research
- Exploration of epigenetic mechanisms in cellular models
Technical Specifications
| Product Name | SGC 0946 |
| Catalog Number | 0957-S7079-10mg |
| CAS Number | 1561178-17-3 |
| Product Type | Small-Molecule Inhibitor |
| Target | Histone Methyltransferase DOT1L |
| Research Area | Epigenetics |
| IC50 | 0.3 nM (cell-free assay) |
| Molecular Formula | C28H40BrN7O4 |
| Size | 10 mg |
| Dry Ice | Yes |
| Hazardous | No |
| Storage Conditions | 2 years at -80°C in solvent |
Chemical Information
Molecular Formula: C28H40BrN7O4
CAS Number: 1561178-17-3
SMILES
Storage and Handling
Store SGC 0946 at -80°C in solvent according to the supplied product specifications. The stated storage stability is up to 2 years under these conditions. Follow the product documentation for solvent preparation, handling and storage recommendations.