BSJ-03-204

BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

Signaling Pathways >> PROTAC >> PROTAC

CDK4/D1:26.9 nM (IC50)

CDK6/D1:10.4 nM (IC50)

BSJ-03-204 (0.0001-100 μM; for 3 or 4 days) has potent anti-proliferative effects on MCL cell lines[1]. BSJ-03-204 (1 μM; for 1 day) potently induces a G1 arrest[1]. BSJ-03-204 (0.1-5 μM; for 4 hours) only resultes in degradation of CDK4/6 in WT cells, not IKZF1/3[1]. Cell Proliferation Assay[1] Cell Line: MCL cell lines (Jeko-1, Mino, Granta-519, Rec-1, and Maver-1 cells) Concentration: 0.0001-100 μM Incubation Time: For 3 or 4 days Result: Had potent anti-proliferative effects on mantle cell lymphoma (MCL) cell lines. Cell Cycle Analysis[1] Cell Line: Granta-519 cells Concentration: 1 μM Incubation Time: For 1 day Result: Potently induced a G1 arrest. Western Blot Analysis[1] Cell Line: Wildtype (WT) or Crbn-/- Jurkat cells Concentration: 0.1, 0.5, 1, 5 μM Incubation Time: For 4 hours Result: Only resulted in degradation of CDK4/6 in WT cells, not IKZF1/3.

[1]. Baishan Jiang, et al. Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6. Angew Chem Int Ed Engl. 2019 May 6;58(19):6321-6326.