HSP90β (C-Terminal Domain) TR-FRET Kit

Products from BPS Bioscience require a minimum order value above 400€

Applications: Screening inhibitors of HSP90β binding for drug discovery and HTS applications. Determine compound IC₅₀.Perform real-time kinetic analyses.

Background: The 90 kDa Heat Shock Proteins (HSP90) are a family of molecular chaperones involved in protein folding and protein degradation. HSP90 can associate with more than 300 substrates, many of which linked to tumorigenesis. HSP90, due to its ability to stabilize proteins linked to cancer progression, has become an attractive target for cancer therapy, with several pan- HSP90 small molecule inhibitors already in clinical trials. However, targeting all HSP90 isoforms has resulted in severe complications. Contrary to the other 3 isoforms, HSP9β is cytosolic and expressed in a constitutive manner, and has more recently become the target of isoform-selective inhibitor drug development.

Contraindications: Keep final DMSO concentration at or below 1%.

Description: The HSP90β (C-terminal domain) TR-FRET Assay Kit is a sensitive high-throughput screening (HTS) TR-FRET Assay Kit designed to measure the inhibition of HSP90β binding to its target protein PPDI in a homogeneous 96-well format or 384-well format. It utilizes a Terbium-labeled donor and a Dye-labeled acceptor to complete the FRET pairing. This TR-FRET based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications.The Terbium-labeled donor will bind to PPDI, while the Dye-labeled acceptor will bind to HSP90β. When PPID is bound to HSP90β TR-FRET occurs and it can be measured using a fluorescence plate reader.

Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed. Avoid multiple freeze/thaw cycles.

Supplied As: 96 reactions: The kit contains enough purified HSP90β (C-terminal Domain) Biotin Labeled, PPDI- GST-tag, labeled donor and acceptor, and assay buffer for 100 reactions. or384 reactions: The kit contains enough purified HSP90β (C-terminal Domain) Biotin Labeled, PPDI- GST-tag, labeled donor and acceptor and assay buffer for 384 reactions.

Uniprot: P08238

Warnings: Avoid freeze/thaw cycles

Biosafety Level: Not applicable (BSL-1)

References: Mishra S., et al. The development of HSP90β-selective inhibitors to overcome detriments associated with pan-HPS90 inhibition. J Med Chem 64 (3), 1545-1557 (2021)Khandelwal A., et al. Structure-guided design of an HPS90β N-terminal isoform-selective inhibitor, Nature Communications 9, 425 (2018)Rahmy S., et al. HSP90β inhibition upregulates interferon response and enhances immune checkpoint blockade therapy in murine tumors, Front Immunol. 13, 10005045 (2022)

• Artikelnummer: BPS50262-1
• Hersteller: BPS Bioscience
• Hersteller Artikelnummer: 50262-1
• Green Labware: Nein
• Verpackungseinheit: 96 reactions
• Mengeneinheit: PAK