Cytochrome P450 2D6 Inhibitor screening

Description: 5'-nucleotidase (5'-NT), also known as ecto-5'-nucleotidase or CD73 (cluster of differentiation 73), is an enzyme that is encoded by the NT5E gene. CD73 commonly serves to convert AMP to adenosine. Ecto-5-prime-nucleotidase (5-prime-ribonucleotide phosphohydrolase) catalyzes the conversion at neutral pH of purine 5-prime mononucleotides to nucleosides, the preferred substrate being AMP. Other forms of 5-prime nucleotidase exist in the cytoplasm and lysosomes and can be distinguished from ecto-NT5 by their substrate affinities, requirement for divalent magnesium ion, activation by ATP, and inhibition by inorganic phosphate. Rare allelic variants are associated with a syndrome of adult-onset calcification of joints and arteries (CALJA) affecting the iliac, femoral, and tibial arteries reducing circulation in the legs and the joints of the hands and feet causing pain.

Description:  A plate based fluorometric assay to screen potential p300 inhibitors in a rapid and high-throughput adaptable way.

Description: The Kynurenine 3-Monooxygenase (KMO) Inhibitor Screening Assay Kit is designed to measure human KMO enzyme inhibition. The kit comes in a convenient format, with enough reaction solution and enzyme to perform a total of 400 reactions. The KMO Inhibitor Screening Assay Kit is simple to use. Recombinant hKMO is mixed with inhibitors and the reaction is initiated through addition of the substrates NADPH and L-Kynurenine. After a room temperature incubation, activity is determined by measuring the absorption of the reaction product at λ=412 nm. The UV absorption signal correlates with the amount of NADPH remaining in the reaction.

Description: The Kynurenine 3-Monooxygenase (KMO) Inhibitor Screening Assay Kit is designed to measure human KMO enzyme inhibition. The kit comes in a convenient format, with enough reaction solution and enzyme to perform a total of 400 reactions. The KMO Inhibitor Screening Assay Kit is simple to use. Recombinant hKMO is mixed with inhibitors and the reaction is initiated through addition of the substrates NADPH and L-Kynurenine. After a room temperature incubation, activity is determined by measuring the absorption of the reaction product at λ=412 nm. The UV absorption signal correlates with the amount of NADPH remaining in the reaction.

Description: The IDE (Insulin-degrading enzyme) Inhibitor Screening Assay is a homogeneous fluorogenic assay designed to measure the activity of IDE for screening and profiling applications. The IDE assay kit comes in a convenient 96-well or 384-well format and contains enough purified IDE (amino acids 71-254), substrate, and PR-02 buffer for 100 or 400 reactions.Figure 1: Illustration of the assay principle.The substrate is an internally quenched fluorogenic substrate. Proteolysis releases the highly fluorescent Mca from the quencher. Fluorescence intensity increases proportionally to the activity of the protease.Need us to run inhibitor screens or profile your compounds against IDE? Check out ourProtease Screening Services.

Description: The IDE (Insulin-degrading enzyme) Inhibitor Screening Assay is a homogeneous fluorogenic assay designed to measure the activity of IDE for screening and profiling applications. The IDE assay kit comes in a convenient 96-well or 384-well format and contains enough purified IDE (amino acids 71-254), substrate, and PR-02 buffer for 100 or 400 reactions.Figure 1: Illustration of the assay principle.The substrate is an internally quenched fluorogenic substrate. Proteolysis releases the highly fluorescent Mca from the quencher. Fluorescence intensity increases proportionally to the activity of the protease.Need us to run inhibitor screens or profile your compounds against IDE? Check out ourProtease Screening Services.

Description: The BRD1 Inhibitor Screening Assay Kit is designed to measure the inhibition of BRD1 binding to its substrate. The key to the BRD1 Inhibitor Screening Assay Kit is the specific binding of the BRD1 bromodomain to the acetylated histone substrate. With this kit, only three simple steps on a microtiter plate are required. First, a sample containing BRD1 and an inhibitor of choice is incubated with the biotinylated substrate for thirty minutes. Next, acceptor beads are added, then donor beads, followed by reading the Alpha-counts.

Description: The CBX1 Inhibitor Screening Assay Kit is designed to measure the inhibition of CBX1 binding to its substrate. The kit comes in a convenient AlphaLISA® format, with enough biotinylated peptide substrate, assay buffer, detection buffer and purified GST-tagged CBX1 chromodomain to perform a total of 384 enzyme reactions. The key to the kit is the specific binding of the CBX1 chromodomain to the methylated-peptide substrate. With this kit, only three simple steps on a microtiter plate are required. First, a sample containing CBX1 and an inhibitor of choice is incubated with the biotinylated substrate for one hour. Next, acceptor beads are added, then donor beads, followed by reading the Alpha-counts.

Description: The USP7 Inhibitor Screening Assay Kit is designed to measure USP7 activity for screening and profiling applications. The USP7 Inhibitor Screening Assay Kit comes in a convenient format, with a 96-well plate, fluorogenic, ubiquitinated substrate, assay buffer, and purified USP7 enzyme for 96 enzyme reactions. USP7 is incubated with a sample containing assay buffer and Ub-AMC Substrate, and then the plate is read, measuring fluorescence using a fluorescence reader.

Description: The CD39 Inhibitor Screening Assay Kit is designed to measure CD39 activity for screening and profiling applications. The CD39 assay kit comes in a convenient 96-well format, with purified recombinant CD39 enzyme, ATP, CD39 assay buffer, and Colorimetric detection reagent for 96 enzyme reactions. In addition, the kit includes the CD39 inhibitor POM-1 for use as an inhibitor control.

Description: The ACE2 Inhibitor Screening Assay Kit is designed to measure the exopeptidase activity of ACE2 for screening and profiling applications. 

Description: The GLS2 Inhibitor Screening Assay Kit is designed to measure the hydrolase activity of GLS2 for screening and profiling applications.

Description: UBE1 dysregulation has been linked to muscular atrophy, tumors, and cancer. The UBE1 Inhibitor Screening Assay Kit is designed to measure UBE1 activity for screening and profiling applications using Kinase-Glo® MAX as a detection reagent. 

Description: The ARG2 Inhibitor Screening Assay Kit is designed to measure ARG2 enzyme inhibition. The kit comes in a convenient format, with enough reaction solution and enzyme to perform a total of 100 reactions. The ARG2 Inhibitor Screening Assay Kit is simple to use. Inhibitor and enzyme are added to a sample containing thioarginine substrate. After a room temperature incubation, activity is determined by measuring the absorption of reaction product at λ=410-415 nm.

Description: The ARG2 Inhibitor Screening Assay Kit is designed to measure ARG2 enzyme inhibition. The kit comes in a convenient format, with enough reaction solution and enzyme to perform a total of 400 reactions. The ARG2 Inhibitor Screening Assay Kit is simple to use. Inhibitor and enzyme are added to a sample containing thioarginine substrate. After a room temperature incubation, activity is determined by measuring the absorption of reaction product at λ=410-415 nm.

Description: The ARG1 Inhibitor Screening Assay Kit is designed to measure ARG1 enzyme inhibition. The kit comes in a convenient format, with enough reaction solution and enzyme to perform a total of 100 reactions. The ARG1 Inhibitor Screening Assay Kit is simple to use. Inhibitor and enzyme are added to a sample containing thioarginine substrate. After a room temperature incubation, activity is determined by measuring the absorption of reaction product at λ=410-415 nm.

Description: The ARG1 Inhibitor Screening Assay Kit is designed to measure ARG1 enzyme inhibition. The kit comes in a convenient format, with enough reaction solution and enzyme to perform a total of 400 reactions. The ARG1 Inhibitor Screening Assay Kit is simple to use. Inhibitor and enzyme are added to a sample containing thioarginine substrate. After a room temperature incubation, activity is determined by measuring the absorption of reaction product at λ=410-415 nm.

Description: The TPH1 Assay Kit is designed to measure TPH1 enzyme inhibition in a 96 reaction format. This fluorescence-based assay kit is especially suitable for high throughput screening applications. The procedure is quick, straightforward, and simple - just mix two solutions, incubate, add quenching solution, and measure the fluorescence.

Description: The TPH2 Assay Kit is designed to measure TPH2 enzyme inhibition in a 96 reaction format. This fluorescence-based assay kit is especially suitable for high throughput screening applications. The procedure is quick, straightforward, and simple -
just mix two solutions, incubate, add quenching solution, and measure the fluorescence.

Description: The CD73 Inhibitor Screening Assay Kit is designed to measure CD73 activity_x000D_for screening and profiling applications. The CD73 assay kit comes in a convenient 96-well_x000D_format, with purified recombinant CD73 enzyme, AMP, CD73 assay buffer, and Colorimetric_x000D_detection reagent for 100 enzyme reactions.

Description: The TPH1 Assay Kit is designed to measure TPH1 enzyme inhibition in a 384 reaction format. This fluorescence-based assay kit is especially suitable for high throughput screening applications. The procedure is quick, straightforward, and simple - just mix two solutions, incubate, add quenching solution, and measure the fluorescence.

Description: The TPH2 Assay Kit is designed to measure TPH2 enzyme inhibition in a 384 reaction format. This fluorescence-based assay kit is especially suitable for high throughput screening applications. The procedure is quick, straightforward, and simple -
just mix two solutions, incubate, add quenching solution, and measure the fluorescence.

Description: The CD73 Inhibitor Screening Assay Kit is designed to measure CD73 activity_x000D_for screening and profiling applications. The CD73 assay kit comes in a convenient 384-well_x000D_format, with purified recombinant CD73 enzyme, AMP, CD73 assay buffer, and Colorimetric_x000D_detection reagent for 384 enzyme reactions.

Description: The USP1 Inhibitor Screening Assay Kit is a 96-well format fluorogenic assay kit designed to measure the activity of the deubiquitinating (DUB) enzyme USP1 (ubiquitin specific peptidase 1) for screening and profiling applications. The kit contains enough purified USP1/UAF1 (ubiquitin specific peptidase 1 associated factor 1) complex, Ubiquitinated-AMC substrate, and assay buffer for 100 reactions.To determine the effect of an inhibitor on USP1 activity, the enzyme should be preincubated with or without the test inhibitor prior to adding the Ub-AMC substrate to the reaction. The assay was functionally validated using Ub-Aldehyde, a potent inhibitor of the DUB subfamilies Ubiquitin C-terminal Hydrolases (UCHs), Ubiquitin-Specific Proteases (USPs), Ovarian Tumor Proteases (OTU), and Machado-Josephin Domain (MJD) proteasesFigure 1: Illustration of the assay principle.Ubiquitin-AMC is a fluorogenic substrate for ubiquitin hydrolases, with a C-terminus derivatization of ubiquitin with 7-amido-4-methylcoumarin (AMC) . In the conjugated form, the energy emitted from fluorochrome AMC is quenched. Upon proteolysis, AMC is no longer quenched and emits fluorescence with an λexcitation/λemission maxima of 350/460 nm. The increase in fluorescence is proportional to the DUB activity.Need us to run inhibitor screens or profile your compounds against USP1? Check out ourProtease Screening ServicesorUbiquitination Screening Services.

Description: The USP5 Inhibitor Screening Assay Kit is a 96-well format fluorogenic assay designed to measure the activity of the deubiquitinating (DUB) enzyme USP5 for screening and profiling applications. The kit contains enough purified USP5 protein, Ubiquitinated-AMC substrate, and assay buffer for 100 reactions.To determine the effect of an inhibitor on USP5 activity, the enzyme should be preincubated with or without the test inhibitor prior to adding the Ub-AMC substrate to the reaction. The assay was functionally validated using Ub-Aldehyde, a potent inhibitor of the DUB subfamilies Ubiquitin C-terminal Hydrolases (UCHs), Ubiquitin-Specific Proteases (USPs), Ovarian Tumor Proteases (OTU), and Machado-Josephin Domain (MJD) proteases.Figure 1: Illustration of the assay principle.Ubiquitin-AMC is a fluorogenic substrate for ubiquitin hydrolases based on the C-terminus derivatization of ubiquitin with 7-amido-4-methylcoumarin (AMC) . In the conjugated form, the energy emitted from the fluorochrome AMC is quenched. Upon proteolysis, AMC is no longer quenched and emits fluorescence with an λexcitation/λemission maxima of 350/460 nm. The increase in fluorescence is proportional to the DUB activity.Need us to run inhibitor screens or profile your compounds against USP5? Check out ourProtease Screening ServicesorUbiquitination Screening Services.

Description: The Ubiquitin specific peptidase 2 (USP2) Inhibitor Screening Assay Kit is a homogeneous fluorogenic assay designed to measure the activity of the deubiquitinating (DUB) enzyme USP2 for screening and profiling applications. The kit contains enough purified USP2 recombinant protein, Ubiquitinated-AMC substrate, and assay buffer for 100 reactions.To determine the effect of an inhibitor on USP2 activity, the enzyme should be preincubated with or without the test inhibitor prior to adding the Ub-AMC substrate to the reaction. The assay was functionally validated using Ub-Aldehyde, a potent inhibitor of DUB subfamilies Ubiquitin C-terminal Hydrolases (UCHs), Ubiquitin-Specific Proteases (USPs), Ovarian Tumor Proteases (OTU), and Machado-Josephin Domain (MJD) proteases.Figure 1: Illustration of the assay principle.Ubiquitin-AMC is a fluorogenic substrate for ubiquitin hydrolases based on the C-terminus derivatization of ubiquitin with 7-amido-4-methylcoumarin (AMC) . In the conjugated form, the energy emitted from fluorochrome AMC is quenched. Upon proteolysis, AMC is no longer quenched and emits fluorescence with an λexcitation/ λemission maxima of 350/460 nm. The increase in fluorescence is proportional to the DUB activity.Need us to run inhibitor screens or profile your compounds against USP2? Check out ourProtease Screening ServicesorUbiquitination Screening Services.