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Background Information:
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.
Reference:
1. G. E. Winter, et al, Phthalimide conjugation as a strategy for in vivo target protein degradation, Science, 2015 Jun 19; 348(6241):1376-81.
APIM050324: DBET1
CAS No.: 1799711-21-9.
Molecular Formula: C38H37ClN8O7S?0.8H2O.
Molecular Weight: 799.7.
Purity: >99.5% (by HPLC at 214 and 254 nm).
QC: HPLC-MS, NMR, and Quantitative Elemental Analysis.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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