Formulation: A solid
Formal Name: (6S)-4-(4-chlorophenyl)-N-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
Purity: ≥98%
Formula Markup: C34H31ClN8O5S
Formula Weight: 699,2
Shelf life (days): 1460
CAS Number: 1883863-52-2
Notes: 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 α (αapp) 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.
English
Deutsch
