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KB02-JQ1

Names

[ CAS No. ]:
2384184-44-3

[ Name ]:
KB02-JQ1

Biological Activity

[Description]:

KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> PROTAC >> PROTAC
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

BRD4


[In Vitro]

KB02-JQ1 (5-40 μM; 24 hours; HEK293T cells) treatment shows concentration-dependent degradation of endogenous BRD4 in HEK293T cells[1]. Western Blot Analysis[1] Cell Line: HEK293T cells Concentration: 5 μM, 10 μM, 20 Μm or 40 μM Incubation Time: 24 hours Result: Concentration-dependent degradation of endogenous BRD4 in HEK293T cells.

[References]

[1]. Zhang X, et al. Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16. Nat Chem Biol. 2019 Jul;15(7):737-746.

Chemical & Physical Properties

[ Molecular Formula ]:
C38H43Cl2N7O6S

[ Molecular Weight ]:
796.76

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds