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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

Prostaglandin D Synthase (hematopoietic-type) FP-Based Inhibitor Screening Assay Kit - Green

Cayman Chemical Item Number 600007

H-PGDS FP-Based Inhibitor Screening Assay Kit - Green; Prostaglandin D Synthase (hematopoietic-type) Fluorescence Polarization-Based Inhibitor Screening Assay Kit - Green

Prostaglandin D Synthase (hematopoietic-type) FP-Based Inhibitor Screening Assay Kit - Green

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Description

Prostaglandin D2 (PGD2) is synthesized by hematopoietic-type PGD-synthase (H-PGDS) in mast cells and is released in large quantities during allergic and asthmatic anaphylaxis. H-PGDS is therefore a key target for development of selective, potent inhibitors for therapeutic use against these diseases. Cayman’s H-PGDS FP-Based Inhibitor Screening Assay Kit - Green provides a rapid, accurate assay for screening H-PGDS inhibitors. In this assay, a H-PGDS inhibitor-fluorescein conjugate serves as a specific fluorescent probe for the enzyme. Displacement of the probe by any unlabeled H-PGDS inhibitor leads to a decrease in the fluorescence polarization (FP) state of the probe, providing a direct signal for binding of the inhibitor to the active site of the enzyme. This assay is robust (Z’ of 0.75) and eliminates the need for the traditional multistep assay that requires the use of highly unstable PGH2. The assay has been validated using several known inhibitors of H-PGDS with IC50 values ranging from nanomolar to millimolar concentrations.
Synonyms
  • H-PGDS FP-Based Inhibitor Screening Assay Kit - Green
  • Prostaglandin D Synthase (hematopoietic-type) Fluorescence Polarization-Based Inhibitor Screening Assay Kit - Green
Stability 6 months
Storage -20°C
Shipping Wet ice in continental US; may vary elsewhere

Background Reading

Kanaoka, Y., Ago, H., Inagaki, E., et al. Cloning and crystal structure of hematopoietic prostaglandin D synthase. Cell 90 1085-1095 (1997).

Zhang, J., Chung, T.D.Y., and Oldenburg, K.R. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 4(2) 67-73 (1999).

Pinzar, E., Miyano, M., Kanaoka, Y., et al. Structural basis of hematopoietic prostaglandin D synthase activity elucidated by site-directed mutagenesis. J Biol Chem 275(40) 31239-31244 (2000).

Inoue, T., Okano, Y., Kado, Y., et al. First determination of the inhibitor complex structure of human hematopoietic prostaglandin D synthase. J Biochem 135 279-283 (2004).

Aritake, K., Kado, Y., Inoue, T., et al. Structural and functional characterization of HQL-79, an orally selective inhibitor of human hematopoietic prostaglandin D synthase. J Biol Chem 281(22) 15277-15286 (2006).

Matsushita, K., Nobutoshi, A., and Hizue, A. Pharmacological studies on the novel antiallergic drug HQL-79: I. Antiallergic and antiasthmatic effects in various experimental models.. Jpn J Pharmacol 78(1) 1-10 (1998).

Matsushita, K., Nobutoshi, A., and Aritake, K. Pharmacological studies on the novel antiallergic drug HQL-79: II. Elucidation of mechanisms for antiallergic and antiasthmatic effects. Jpn J Pharmacol 78(1) 11-22 (1998).

Hohwy, M., Spadola, L., Lundquist, B., et al. Novel prostaglandin D synthase inhibitors generated by fragment-based drug design. J Med Chem 51 2178-2186 (2008).

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600007-384well
384-Well Solid Plate (black; non-binding)
Foil Plate Covers
H-PGDS FP Assay Fluorescent Probe - Green 1 ea
H-PGDS (human recombinant) FP Assay Reagent 1 ea
HQL-79 FP Positive Control 1 ea
FP Assay Buffer Concentrate (4X) 1 ea
H-PGDS FP Glutathione 1 ea
600007-1920well
384-Well Solid Plate (black; non-binding)
Foil Plate Covers
H-PGDS FP Assay Fluorescent Probe - Green 5 × 1 ea
H-PGDS (human recombinant) FP Assay Reagent 5 × 1 ea
HQL-79 FP Positive Control 5 × 1 ea
FP Assay Buffer Concentrate (4X) 5 × 1 ea
H-PGDS FP Glutathione 5 × 1 ea
Size Price Quantity Subtotal
384 wells $356.00 $0.00
1,920 wells $1,335.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-02-10. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

You may be eligible to receive a free sample Prostaglandin D Synthase (hematopoietic-type) FP-Based Inhibitor Screening Assay Kit - Green under the Cayman Challenge program.

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Prostaglandin D Synthase Inhibitor Screening Assay Kit
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UltraPure Water
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