Functional Assays

The SetDB1 Chemiluminescent Assay Kit is designed to measure SetDB1 activity for screening and profiling applications. The advantage of the SetDB1 Chemiluminescent Assay Kit is a highly specific antibody that recognizes the methylated K9 residue of Histone H3. With this kit, only three simple steps are required. First, S-adenosylmethionine is incubated with a sample containing the assay buffer and the methyltransferase enzyme. Next, the primary antibody is added. Finally, the wells are treated with an HRP-labeled secondary antibody followed by addition of the HRP substrate to produce chemiluminescence that can be measured using a chemiluminescence reader.

The CDK12/ Cyclin K Kinase Assay Kit is designed to measure the activity of complex CDK12/ Cyclin K for screening and profiling applications using luminescent Kinase-Glo® MAX as a detection reagent.

BRAF is a serine-threonine kinase activated by the RAS GTPases in response to growth factor stimulation or oncogenic insult. Upon stimulation, BRAF phosphorylates the kinase MEK1 (dual specificity mitogen-activated protein kinase kinase 1), resulting in the activation of the MAP-kinase (mitogen-activated protein) cascade. The MAP-kinase signaling pathway controls cell growth, and dysregulation of this pathway is frequently observed in cancer. Inherited BRAF mutations cause birth defects, while cancer-associated mutations are frequently observed in melanoma. BRAF is a validated therapeutic target for anti-cancer drugs, notably in melanoma. The BRAF (WT) Kinase Assay Kit is designed to measure BRAF(WT) kinase activity for screening and profiling applications using Kinase-Glo® MAX as a detection reagent. 

The 3CL Protease (B.1.1.529, Omicron Variant) (SARS-CoV-2) Assay Kit is designed to measure the activity of P132H mutated, Omicron variant 3CL Protease for screening and profiling applications, in a homogeneous assay with no time-consuming washing steps. The 3CL Protease Substrate is an internally quenched 14-mer fluorogenic (FRET) peptide (DABCYL-KTSAVLQSGFRKME-EDANS). When the donor (EDANS) and acceptor (DABCYL) fluorophores are in close proximity, the energy emitted from EDANS is quenched by DABCYL (intact substrate). Upon proteolysis by 3CL, the peptide substrate is cleaved between glutamine and serine to generate the highly fluorescent peptide fragment (SGFRKME-EDANS). The fluorescence intensity increases proportionally to the activity of 3CL. More information on the substrate, including MW and structure, can be found on our website (BPS Bioscience, #79952).

Please note this product may be subject to fees, we invite you to contact your local office. 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.

TTK, also known as Monopolar Spindle 1 Kinase (MPS-1), is a dual specific kinase (tyrosine and serine/threonine) that plays an important role in the cell division cycle by regulating spindle assembly checkpoint during mitosis. Recent studies showed that inhibition of TTK induces aberrant mitosis and apoptosis in various cancer cells, suggesting that TTK is a potential cancer therapeutic target. The TTK Kinase Assay Kit is designed to measure TTK kinase activity for screening and profiling applications using ADP-Glo® Kinase Assay as a detection reagent. 

The Spike S1 RBD (B.1.1.529 BA.1, Omicron Variant) (SARS-CoV-2): ACE2 Inhibitor Screening Chemiluminescence Assay Kit is designed for screening and profiling neutralizing antibodies or inhibitors of the interaction between the Omicron variant SARS-CoV-2 Spike RBD and human ACE2. This kit comes in a convenient 96-well format, with Biotinylated-ACE2, purified Spike RBD (Omicron Variant; B.1.1.529 BA.1) protein, Streptavidin-HRP, and assay buffers for 100 reactions.  The assay requires only a few steps. First, SARS-CoV-2 Spike RBD (Omicron Variant; B.1.1.529 BA.1) is coated on a 96-well plate overnight. After washing and blocking, the protein is pre-incubated with an inhibitor or neutralizing antibody. Upon subsequent incubation with Biotin-ACE2, the plate is treated with Streptavidin-HRP followed by addition of a chemiluminescence HRP substrate to produce the luminescence signal.

The Spike S1 (B.1.1.529 BA.1, Omicron Variant) (SARS-CoV-2): ACE2 TR-FRET Assay is designed to measure the inhibition of the binding between SARS-CoV-2 Spike S1 (B.1.1.529 BA.1, Omicron Variant) and human ACE2 in a homogeneous 384 reaction format. This TR-FRET-based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications. The assay procedure is straightforward and simple; the test inhibitor compound is incubated with biotinylated Spike S1, Eu-labeled ACE2, and the dye-labeled acceptor for one hour. Then the TR-FRET signal is measured using a fluorescence reader capable of measuring Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET).

The ULK1 Kinase Assay Kit is designed to measure ULK1 activity for screening and profiling applications, using Kinase-Glo® MAX as a detection reagent.