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Potent and selective BCL6 degrader that targets BTB domain with high-affinity.
BI-3802 is a potent and selective BCL6 degrader that targets BTB domain with high-affinity (IC50 ≤3 nM by ULight assay). BI-3802 induces BCL6 polymerization (filaments formation) and SIAH1 E3 ligase-mediated ubiquitination, leading to proteasomal degradation (by 80% post 90 min 5 µM treatment in SU-DHL-4 cells) and inhibition of BCL6-dependent proliferation in a dose-depenent manner (typical dosing range 0.04 - 3 µM).
BI-3802 is a potent and selective BCL6 degrader that targets BTB domain with high-affinity (IC50 ≤3 nM by ULight assay). BI-3802 induces BCL6 polymerization (filaments formation) and SIAH1 E3 ligase-mediated ubiquitination, leading to proteasomal degradation (by 80% post 90 min 5 µM treatment in SU-DHL-4 cells) and inhibition of BCL6-dependent proliferation in a dose-depenent manner (typical dosing range 0.04 - 3 µM).
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