Microsomal Prostaglandin E2 Synthase-1 (mPGES-1), with cyclooxygenase-2 (COX-2), synthesizes PGE2, which is directly involved in signaling during inflammation, fever and pain. 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs), which are pro-inflammatory mediators. CAY10589 is a dual inhibitor of mPGES-1 (IC50 = 1.3 μM) and 5-LO (IC50 = 1.0 μM). It effectively inhibits PGE2 and LT synthesis in both cell free and intact cell assays. CAY10589 has minor effects on COX-1 and COX-2, inhibiting these enzymes 34% and 38.8%, respectively, at 10 μM.
Uses
CAY10589 is an inhibitor of mPGES-1, an enzyme induced during inflammatory responses. CAY10589 has no significant effect on the differentiation of BM myeloid precursor cells into M2-like TAMs[1][2].
Definition
ChEBI: CAY10589 is a member of biphenyls.
storage
Store at -20°C
References
[1] Wiegard A, et al. Pyrrole alkanoic acid derivatives as nuisance inhibitors of microsomal prostaglandin E2 synthase-1. Eur J Med Chem. 2012 Feb;48:153-63. DOI:10.1016/j.ejmech.2011.12.009 [2] Li L, et al. Targeting the lipid metabolic reprogramming of tumor-associated macrophages: A novel insight into cancer immunotherapy. Cell Oncol (Dordr). 2023 Sep 30. DOI:10.1007/s13402-023-00881-y
