PROTAC® Optimization Kit for CDK Kinase-Cereblon Binding
BPS-79924 384 reactions
Data Sheet: 
Applications
Identify and optimize PROTACs targeting the CDK family of kinases.
Design novel molecules targeting CRBN.
Directly compare the activity of different PROTACs.
Shipment
-80°C (dry ice)
Literature References
Brand M., et al., 2019 Cell Chem. Biol. 26(2):300-306.
Nunes J., et al., 2019 ACS Med Chem Lett 10(7): 1081-1085.
Łukasik P., et al., 2021 Int J Mol Sci. Mar 13;22(6):2935.
Description
The PROTAC® Optimization Kit for CDK-Cereblon Binding is designed for the testing and profiling of PROTACs (proteolysis targeting chimera) directed against the CDK (Cyclin-dependent kinase) protein family and Cereblon (CRBN). The PROTAC® Optimization Kit for CDK-Cereblon Binding comes in a convenient AlphaLISA® format, with enough BSJ-03-204 PROTAC®, CDK PROTAC® buffer, purified CDK4/Cyclin D3, CDK6/Cyclin D3, and CRBN for 400 reactions. The CDK inhibitor Palbociclib is included as a control inhibitor of PROTAC binding to CDK (internal control). The PROTAC® of interest is incubated with CRBN and CDK4 or CDK6, bringing them in close proximity. CDK contains an His-tag, which is recognized by the Ni donor bead. Biotinylated cereblon binds to the Streptavidin AlphaLISA™ acceptor bead. Upon excitation of the donor bead, a singlet oxygen is generated by the donor bead. The singlet oxygen excites the acceptor bead, which emits light proportionally to the level of interaction. - Identify and optimize PROTACs targeting the CDK family of kinases.
Design novel molecules targeting CRBN.
Directly compare the activity of different PROTACs. - BSJ-03-204 is a thalidomide-derivative, which is known to cause severe birth defects in humans. It is very important to use all appropriate precautions when handling this compound. Avoid freeze/thaw cycles.
ESCLUSIVAMENTE PER USO DI RICERCA (RUO) e non per uso terapeutico o diagnostico su uomini o animali. Il prodotto NON è un Dispositivo Medico o un Diagnostico in Vitro.
PRODUCT FOR RESEARCH USE ONLY (RUO) and not for therapeutic or diagnostic use on humans or animals. The product is NOT a Medical Device or an In-Vitro Diagnostic (IVD).
