dBET1 etin Gabapentin dose-dependently (10-100 mg/kg

Gabapentin dose-dependently (10-100 mg/kg

under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold

Epub 2013 Feb 7

Formula: C12H17N5O4

dBET1 etin Gabapentin dose-dependently (10-100 mg/kgdBET1 is a potent BRD4 degrader (IC50=20 nM), and competitive antagonist of BET bromodomains to hijack the Cereblon E3 ubiquitin ligase complex. dBET1 is a hybrid molecule that combines (+) JQ1 and thalidomide. 1 The JQ1 portion facilitates binding of dBET1 to the bromodomains of BET family transcriptional activators. The thalidomide moiety drives proteasomal degradation, as phthalimides bind cereblon to create a substrate recognition site for E3