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BI 894999
BI 894999 is a small molecule oral BET inhibitor suitable for in vitro and in vivo studies. BET family proteins are key regulators of transcription. The related molecule BI-6953 is available as a negative control.
ACBI2
ACBI2 is a highly potent (DC50, 18h, RKO SMARCA2 = 1 nM) and orally bioavailable (Foral, mice = 22%) SMARCA2-VHL PROTAC. ACBI2 shows selective degradation of SMARCA2 over SMARCA4 in ex vivo human whole blood assays and in vivo efficacy in SMARCA4-deficient cancer models.
BI-7190
BI-7190 is a probe to study the impact of BPTF bromodomain inhibition in vitro and in vivo. BPTF is a core component of the nucleosome remodelling factor (NURF) complex. BI-7190 binds with high affinity to the bromodomain of BPTF KD (BPTF, DiscoveRx) = 3.5 nM, displays good cellular potency EC50 (BPTF, nanoBRET) = 58, and selectivity to …
VZ185
VZ185 is a first-in-class low-molecular-weight VHL-based PROTAC (proteolysis-targeting chimera) degrader of the BAF/PBAF complexes subunits BRD7 and BRD9. It tethers our probe BI-7273, which is a potent and selective ligand for the BRD7/9 bromodomains, to the VHL E3 ubiquitin ligase ligand VH101, aimed at triggering the intracellular …