BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78.
BSJ-05-037 induces potent degradation of ITK dependent on CRBN, neddylation, and the proteasome.
BSJ-05-037 induces GATA-3 loss and decreases chemotherapy resistance in vitro.
BSJ-05-037 disrupts TCR signaling, downregulates the Th2-associated transcription factor GATA-3, and can overcome chemotherapy resistance in TCL models in vivo.
