dBET6

dBET6

CAT N°: 35385
Price:

From 129.00 109.65

dBET6 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4).{63349} It is characterized as a proteolysis-targeting chimera (PROTAC) and contains JQ1, which binds bromo- and extra-terminal (BET) proteins, linked to thalidomide, a ligand for the E3 ubiquitin ligase cereblon.{63350} dBET6 binds to BRD4 (IC50 = 14 nM) and induces its degradation when used at a concentration of 100 nM, leading to a global inhibition of transcription in MOLT-4 T cell acute lymphoblastic leukemia (T-ALL) cells.{63349} It also reduces leukemic burden in a MOLT-4 T-ALL mouse xenograft model when administered at a dose of 7.5 mg/kg twice per day.

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