dBET57

dBET57

CAT N°: 36626
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From 43.00 36.55

dBET57 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4).{64614} It is characterized as a proteolysis-targeting chimera (PROTAC) and contains JQ1, which binds bromo- and extra-terminal domain (BET) proteins, linked to thalidomide, a ligand for the E3 ubiquitin ligase cereblon. dBET57 is selective for inhibiting the interaction between cereblon and bromodomain 1 of BRD4 (BRD4BD1) over the interaction between cereblon and BRD4BD2 with apparent cooperativity factor ? (?app) values of 0.8 and less than 0.1, respectively, in an assay using purified bromodomains. It reduces BRD4BD1 protein levels in vitro with a half-maximal degradation (DC50) value of approximately 500 nM after five hours but does not reduce levels of BRD4BD2.

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