PC1002: dBET1

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SKU: PC-1002 Categories: ,

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

 

Additional information

Weight

5 mg, 10 mg, 25 mg

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dBET is a JQ1 based PROTAC that selectively degrades BRD4 in cells