Products from BPS Bioscience require a minimum order value above 400€
Application: Screen small molecule inhibitors or antagonists that affect KRAS Isoform B nucleotide-binding status in high throughput (HTS) applications. Counter-screen compounds that affect mutated forms of KRAS.
Background: High levels of wild-type KRAS cause a slowing of cell replication and growth, and increased apoptosis. This can be induced by cellular stress, certain types of radiation, chemical signals, and other prompts. Wild-type KRAS may also protect against mutant KRAS over-activation by dimerizing with mutant KRAS protein. The study of differences in the behavior of the wild-type and mutated forms of KRAS is especially important since KRAS mutations are responsible for more than 30% of human cancers. Compounds that affect the nucleotide exchange (GDP to GTP) reaction provide a novel approach to the inhibition of tumor cell growth in KRAS-driven tumors. In 2021, the Food and Drug Administration (FDA) granted approval for use of AMG510 (Sotorasib), a potent KRAS G12C inhibitor for non-squamous non-small cell lung cancer.
Contraindications: This kit is compatible with up to 1% final DMSO concentration. Compounds that are fluorescent may interfere with the results, depending on their spectral excitation and emission properties. It is recommended that the compound alone is tested to determine any potential interference of the compound on the assay results.
Description: The KRAS Isoform B Coupled Nucleotide Exchange TR-FRET Assay Kit is a TR-FRET (Time-Resolved Fluorescence Resonance Energy Transfer) assay kit designed for screening and profiling of KRAS Isoform B antagonists/inhibitors. It monitors the binding of an effector protein such as the Ras binding domain of RAF1, (RBD-cRaf) to KRAS. The KRAS Isoform B Coupled Nucleotide Exchange TR-FRET Assay Kit comes in a convenient 384-well format, with enough purified recombinant GDP-loaded KRAS Isoform B, GTP, exchange factor SOS1 (son of sevenless homolog 1) (amino acids 564-1049), an effector protein RBD-cRAF (amino acids 50-140), assay buffer and additives for 400 reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Uniprot: P01116
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
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