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BSJ-04-132

Names

[ CAS No. ]:
2349356-39-2

[ Name ]:
BSJ-04-132

Biological Activity

[Description]:

BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> CDK
Signaling Pathways >> PROTAC >> PROTAC

[Target]

CDK4/D1:50.6 nM (IC50)

CDK6/D1:30 nM (IC50)


[In Vitro]

BSJ-04-132 (0.1-5 μM; for 4 hours) only resultes in degradation of CDK4 in WT cells, not CDK6 and IKZF1/3[1]. 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 in WT cells, not CDK6 and IKZF1/3.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C42H49N11O7

[ Molecular Weight ]:
819.91

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds