Novel amide and imidazole compounds as potent hematopoietic prostaglandin D2 synthase inhibitors

news February 25 2021

 

Cayman chemists develop a cell-active, PGD2-competitive inhibitor with low nM affinity for H-PGDS that obeys the rule of five.

 

Highlights

  • Potent, long-lived inhibition of hematopoietic prostaglandin D2 synthase (H-PGDS) has potential as a therapeutic for a variety of inflammatory diseases including asthmatic anaphylaxis, mastocytosis, rheumatoid arthritis, and Duchenne muscular dystrophy.
  • KMN-010034 was identified as a low nM inhibitor of H-PGDS from a targeted series of 20 compounds evaluated by a competitive binding assay, a direct binding assay, a kinetic inhibition assay, and a cell-based ELISA.
  • This novel imidazole analog displays an increase in competition with glutathione (GSH) for the H-PGDS active site, compared to amide-linker analogs previously generated from pharma programs such as Sanofi’s that are not competitive with GSH. The significance of this will be explored in a future publication.

 

Products Related to This Research

Prostaglandin D2 ELISA Kit

  • Measure PGD2 in multiple sample types
  • Assay 24 samples in triplicate or 36 samples in duplicate
  • Measure PGD2 levels down to 55 pg/ml
  • Incubation: 18 hours | Development: 90-120 minutes

| Read: Colorimetric at 405-420 nm

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

  • Screen for inhibitors of H-PGDS
  • Designed for high-throughput screening
  • Includes HQL-79 as a positive control
  • Plate-based fluorescence polarization measurement (ex 470 nm, em 530 nm)

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