PC1002: dBET1

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