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hPGDS-IN-1

hPGDS-IN-1
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Purity:100%
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hPGDS-IN-1

Catalog No. T2681Cas No. 1234708-04-3
hPGDS-IN-1 is a hPGDS inhibitor.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePrice/USDAvailabilityQuantity
1 mg$115In Stock
5 mg$247In Stock
10 mg$372In Stock
25 mg$629In Stock
50 mg$896In Stock
100 mg$1,220In Stock
500 mg$2,450In Stock
1 mL x 10 mM (in DMSO)$272In Stock
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Product Introduction

Bioactivity
Description
hPGDS-IN-1 is a hPGDS inhibitor.
Kinase Assay
TR-FRET biochemical assay with MET wild type and mutants: Enzyme activity is measured in a time resolved fluorescence resonance energy transfer (TR-FRET) assay, detecting tyrosine phosphorylation with a Eu-labelled anti-phospho-tyrosine antibody (fluorescence donor) and Allophycocyanin conjugated to Streptavidin (fluorescence acceptor) which binds to a biotin on the substrate peptide. For each variant, Km concentrations for ATP are determined in the absence of NVP-BVU972, and the ATP concentration in the kinase reaction is set to Km (4 μM for MET wt, 1 μM for MET Y1230H and MET F1200I). NVP-BVU972 is dissolved and diluted in DMSO and assayed in quadruplicate. Kinase reactions are carried out in 50 mM Tris-HCl pH 7.5, 8 mM MgCl2, 4 mM MnCl2, 0.05 % Tween 20, 0.05% bovine serum albumin, 0.1 mM EDTA, 1 mM DTT, 0.1 mM Na3VO4, in white 1536 well plates at room temperature. NVP-BVU972 and enzyme are incubated in a volume of 2 μL for 20 min, followed by the addition of 1 μL ATP and 1 μL biotinylated peptide substrate (PTK1) to final concentrations of Km and 1 μM, respectively. Enzyme concentrations in the reactions are 5 nM for MET wt, and 4 nM for the F1200I and Y1230H variants. After 90 min, reactions are stopped by addition of 1 μL stop/detection solution to reach final concentrations of 10 mM EDTA, 3.5 nM Eu-labelled antiphospho-tyrosine antibody PY20, and 10 nM Streptavidin Allophycocyanin. Time resolved fluorescence resonance energy transfer is measured in an Envision plate reader (excitation 320 nm, emission 615 nm and 665 nm).
Chemical Properties
Molecular Weight416.43
FormulaC22H20N6O3
Cas No.1234708-04-3
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 30 mg/mL (72.04 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4014 mL12.0068 mL24.0136 mL120.0682 mL
5 mM0.4803 mL2.4014 mL4.8027 mL24.0136 mL
10 mM0.2401 mL1.2007 mL2.4014 mL12.0068 mL
20 mM0.1201 mL0.6003 mL1.2007 mL6.0034 mL
50 mM0.0480 mL0.2401 mL0.4803 mL2.4014 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μLDMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μLDMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μLTween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify.
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