BCL6 PROTAC
Molecular Target
B Cell Lymphoma 6 (BCL6)
E3 Ligase
Cereblon (CRBN)
Biological Role
Master transcriptional regulator which leads the differentiation of naive helper T-cells in Follicular Helper T-cells (TFH cells)
Activity
IC50 =120nM FRET affinity and cellular activity. This is a well characterised probe with excellent proteome pull-down selectivity. In vitro studies showed that the BCL6 PROTAC was able to access and equally degrade BCL6 in all cellular compartments. The overall target degradation was estimated to be ~80%. The BCL6 PROTAC demonstrated good in vitro DMPK properties, but was not tested in vivo.