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Overview
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dBET1 is a novel, potent, and competitive CRBN-based BET degrader (PROTAC) with an IC50 of 20 nM. It exhibits high selectivity among 7,429 proteins, only the expression of the oncoproteins MYC and PIM1, as well as BRD2, BRD3 and BRD4 are significantly downregulated by dBET1 treatment. BET degradation with dBET1 will likely reduce expression of pro-inflammatory genes in in vivo neuroinflammatory models associated with microglial/immune cell activation.
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- Properties
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Overview