CCT367766

CCT-367766 (CCT367766) is a novel heterobifunctional PROTAC that binds and degrades the putative transcription factor regulator Pirin in cells.

Research Areas >> Cancer

Signaling Pathways >> PROTAC >> PROTAC

CRBN-DDB1:490 nM (IC50)

CCT367766 (50-1500 nM; 24 hours) demonstates the depletion of pirin protein as a the time-dependent hook-effect in SK-OV-3 human ovarian cancer cells[1]. CCT367766 (0.5-50 nM; 2 hours) demonstrates the concentration-dependent depletion of pirin protein after 2 h exposure in SK-OV-3 cells[1]. Western Blot Analysis[1] Cell Line: SK-OV-3 human ovarian cancer cells Concentration: 50, 150, 250, 500 and 1500 nM Incubation Time: 2 hours, 4 hours, 24 hours Result: Decreased pirin protein expression. Western Blot Analysis[1] Cell Line: SK-OV-3 human ovarian cancer cells Concentration: 0.5, 1, 2.5, 5, 7.5, 10, 25, and 50 nM Incubation Time: 2 hours Result: Completely degraded pirin just at 50 nM treatment.

[1]. Chessum NEA, et al. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).J Med Chem. 2018 Feb 8;61(3):918-933.