BCL-XL TR-FRET Assay Kit

The BCL-XL TR-FRET Assay Kit is designed to measure the inhibition of BCL-XL (B-cell lymphoma-extra large) binding to its ligand in a Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) homogeneous format. This FRET-based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications. This kit contains enough recombinant BCL-XL, BCL-XL peptide ligand, assay buffer, Anti-His Terbium-Labeled Donor, and Dye-labeled Streptavidin Acceptor for 400 reactions.Need us to run inhibitor screens or profile your compounds against BCL-XL? Check out ourApoptosis Screening Services.

Product Specifications

Background

BCL-XL (B-cell lymphoma-extra large), also called BCL2L1, is a member of the BCL-2 family of proteins and is involved in regulating apoptosis. BCL-XL is part of the group of BCL-2 proteins considered pro-survival proteins, as when bound to their effector proteins they inhibit apoptosis. BCL-XL plays a role in the permeability of mitochondrial membrane, allowing the release of cytochrome C. In addition to its role in apoptosis, it is also involved in neural growth, synaptic plasticity, and neuroprotection. As their name indicates, they are found at abnormal levels in B-cell lymphoma and may contribute to the progression of the disease. BCL-XL overexpression is found in about 80% of lymphomas, and it is thus an attractive target in cancer therapy. Recently it has been identified as being a player in autoimmune disorders and ageing, by controlling the apoptosis rate of immune cells, fibroblasts and other cell types. Several therapeutic approaches have been explored to target BCL-XL, ranging from small inhibitors, such as navitoclax, to PROTACs (proteolysis targeting chimeras) . PROTAC 753B, a PROTAC targeting BCL-XL/BCL2 to VHL (von Hippel-Lindau), has been shown to increase the effects of chemotherapy, while avoiding off-target effect on platelets, as these do not express VHL. Advances in small inhibitors are also ongoing and promise to bring benefit to oncologic patients.

UniProt

Q07817

Applications

Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.

Format

96 WellCatalog #NameAmountStorage50273BCL-XL, His-Tag*2.1 µg-80°C30058BCL-XL Peptide Ligand, Biotin-Labeled25 µl-80°CAnti-His Terbium-Labeled Donor10 µl-20°CDye-labeled Streptavidin Acceptor10 µl-20°C300593x BCL TR-FRET Assay Buffer4 ml-20°C79696White, nonbinding, low volume microtiter plate1Room Temp*The concentration of the protein is lot-specific and will be indicated on the tube.384 WellCatalog #NameAmountStorage50273BCL-XL, His-Tag*4.2 µg-80°C30058BCL-XL Peptide Ligand, Biotin-Labeled50 µl-80°CAnti-His Terbium-Labeled Donor2 x 10 µl-20°CDye-labeled Streptavidin Acceptor2 x 10 µl-20°C300593x BCL TR-FRET Assay Buffer2 x 4 ml-20°C79696White, nonbinding, low volume microtiter plate1Room Temp*The concentration of the protein is lot-specific and will be indicated on the tube.

Shipping Conditions

-80°C (Dry Ice)

Storage Conditions

Stable at least 6 months from date of receipt, when stored as directed. Kit components require different storage conditions. Be sure to store each component at the proper temperature upon arrival.