Specifications
dBET1 is a potent and selective BRD4 protein degrader. The molecule, dubbed “degronimid”, is harnessed by combining two specific high affinity protein ligands, (+)-JQ1 for BRD4 and Phthalimide for E3 ubiquitin ligase cereblon (CRBN), tethered by a linker. Fully exploiting the cells’ own protein-degrading machinery, the molecule drags the ubiquitin ligase complex into the tagged protein, leading to a fast, sustainable, CRBN-dependent and ligand-guided BRD4 degradation. It is so selective that only three proteins, BRD2, 3, 4, of >7000 within the cell, were affected. dBET1 demonstrated powerful anti-leukemia activities both in cell and in animal model, with few noticeable side effects.
Info
| Purity | >99.5% |
| Quantity | 5 mg, 10 mg, 25 mg |
| Molecular Weight | 799.7 g/mol |
| Physical State | Lyophilized white powder |
| Solubility | 40 mg/mL in DMSO |
| CAS No. | 1799711-21-9 |
| Storage | solutions at -20°C or -80°C; desiccated at -20°C, avoid freeze/thaw cycles |
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