Prostaglandin D Synthase (hematopoietic-type) FP-Based Inhibitor Screening Assay Kit - Green_上海惠诚生物生物试剂,标准品,仪器设备,耗材,一站式服务

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Cat. Number

065902613130186

Chemical Name

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

References

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	Global Purchasing
384 wells
1,920 wells

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.

下一个：Prostaglandin D2 FPIA Kit - Red上一个：Prostaglandin D Synthase (hematopoietic-type; human recombinant)

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