PARP1 Olaparib Competitive Inhibitor Assay Kit

  BPS-82293 96 reactions

Data Sheet:    

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Screen molecules that bind to PARP1 in the same binding site as Olaparib for drug discovery high-throughput screening (HTS) applications. Determine IC₅₀ values of PARP1 inhibitors with the same binding site as Olaparib.  

-80°C (dry ice)  

Marques M., et al., 2019 Oncogene 38 (12): 2177-2191.  

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Description

 

The PARP1 Olaparib Competitive Inhibitor Assay Kit is a competitive FP (fluorescent polarization) assay designed to measure the formation of a complex between PARP1 (poly(ADP-ribose) polymerase 1) and a fluorescent probe that contains the PARP1 inhibitor Olaparib. When the probe is bound to PARP1, FP is high. In the presence of a test compound able to bind to the same site in PARP1 as Olaparib, the Olaparib-containing fluorescent probe is displaced from PARP1 and remains in solution, resulting in low FP. The PARP1 Olaparib Competitive Inhibitor Assay Kit comes in a convenient 96-well format, with purified PARP1 enzyme, Olaparib-containing fluorescent-labeled probe, and assay buffer for 100 enzyme reactions. Note: This kit is not appropriate for inhibitors expected to bind to PARP1 at different sites from Olaparib. PARP1 binds to the Olaparib-containing fluorescent probe, forming a complex. This complex, when subjected to polarized excitation light, emits highly polarized light due to its restricted movement in solution. In the presence of a test compound (A), PARP1 may form a complex with either the test compound, if the compound has the same binding site of PARP1 as Olaparib, or with the Olaparib-containing fluorescent probe. If the test compound binds to PARP1 at the same site, the Olaparib-containing fluorescent is freed and a decrease in FP is observed. The decrease in FP value is proportional to the competitive binding of the test compound to PARP1. This assay requires a fluorescent microplate reader capable of measuring fluorescence polarization (FP) to read the FP signal. For more information FP technology, visit our Tech Note: FP, assay principles and applications.  - Screen molecules that bind to PARP1 in the same binding site as Olaparib for drug discovery high-throughput screening (HTS) applications. Determine IC₅₀ values of PARP1 inhibitors with the same binding site as Olaparib. - This assay requires a fluorescent microplate reader capable of measuring fluorescence polarization (FP) and equipped with the required parts to read the FP signal. For more information FP technology, visit our Tech Note: "FP, assay principles and applications", bpsbioscience.com/fluorescence-polarization-assays-principles-applications Avoid freeze/thaw cycles