Products from BPS Bioscience require a minimum order value above 400€
Applications: Study enzyme kinetics and screen small molecular inhibitors for drug discovery and High Throughput (HTS) applications.
Background: It is well established that RAS mutations are responsible more than 30% of human cancers. KRAS(G12D) is one of the KRAS mutations that is found frequently in pancreatic and colon cancers. Recent studies have led to the discovery of a small molecule called MRTX-1133 that locks KRAS conformation in the GDP-bound state, thereby blocking KRAS(G12D)-mediated signaling pathway. Compounds that affect the nucleotide exchange (GDP to GTP) reaction in KRAS could lead to a novel approach to the inhibition of tumor cell growth in KRAS(G12D)-driven tumors.
Description: The KRAS(G12D) Nucleotide Exchange Assay is a homogeneous assay designed for the screening and profiling of KRAS(G12D) antagonists/inhibitors by using BODIPY-GDP to monitor the GDP or GTP binding status. The kit can be used with two different protocols for greater flexibility, either titrating the inhibitor at a fixed GTP concentration or titrating the GTP at a fixed inhibitor concentration.BODIPY® FL GDP, is a mixed isomer in which the BODIPY® FL fluorophore has been attached to the 2' or 3' position of the ribose ring via a linker. BODIPY® FL dye is a green-fluorescent dye with similar excitation and emission to fluorescein or Alexa Fluor™ 488. It is characterized by a high extinction coefficient and high quantum yield and is relatively insensitive to pH changes. The dye has an excited-state lifetime of 5 nanoseconds or longer, ideal for fluorescence polarization-based assays.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Supplied As: The KRAS(G12D) Nucleotide Exchange Assay Kit comes in a convenient 384-well format, with enough purified recombinant KRAS(G12D) labeled with BODIPY-GDP, GTP, assay buffer and additives for 400 enzyme reactions.
Uniprot: P01116
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
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