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Applications: Great for identifying and optimizing PROTACs targeting the CDK family of kinases, the design of novel molecules targeting CRBN, and comparison of activities of different PROTACs.
Contraindications: Green and blue dyes that absorb light in the AlphaScreen signal emission range (520-620 nm), such as Trypan Blue. Avoid the use of the potent singlet oxygen quenchers such as sodium azide (NaN3) or metal ions (Fe2+, Fe3+, Cu2+, Zn2+ and Ni2+). The presence of culture medium RPMI 1640 at >1% leads to signal reduction due to the presence of excess biotin and iron in this medium. MEM, which lacks these components, does not affect AlphaScreen assays.
Description: The PROTAC Optimization Kit for CDK Kinase-Cereblon Binding is designed for testing and profiling of PROTACs directed against the CDK Kinase family and Cereblon. Cereblon (CRBN) is a Substrate recognition component of the DCX (DDB1-CUL44-Rbx1) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins.
The CDK inhibitor Palbociclib is included as a control inhibitor of PROTAC binding to CDK. With this kit, only three simple steps on a microtiter plate are required for PROTAC activity detection. First, a sample containing PROTAC is incubated with CRBN and CDK4 or CDK6 Kinase. Next, acceptor beads are added, then donor beads, followed by reading the Alpha-counts.
Storage Stability: At least six months from date of receipt when stored as directed.
Supplied As: The PROTAC Optimization Kit for CDK Kinase-Cereblon Binding comes in a convenient AlphaLISA® format, with BSJ-03-204 PROTAC, CDK PROTAC buffer, purified CDK4 and CDK6, and CRBN for 384 reactions.
Warnings: 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.
Biosafety Level: Not applicable (BSL-1)
References: Brand, M., et al. Cell Chem. Biol. 2019; 26(2):300-306.