PeptideDB

CAY10526

CAS No.: 938069-71-7

CAY10526 (BTH) is a selective mPGES-1 inhibitor that acts as an inhibitor of the NF-κB signaling pathway.
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Description CAY10526 (BTH) is a selective mPGES-1 inhibitor that acts as an inhibitor of the NF-κB signaling pathway.
In vitro CAY10526 dose-dependently inhibits PGE2 production in lipopolysaccharide-stimulated RAW 264.7 cells with an IC50 value of 1.8 μM without any effect on COX-2 expression[1].
Target activity mPGES-1:1.8 μM
Synonyms CAY-10526, BTH, CAY 10526
molecular weight 311.15
Molecular formula C12H7BrO3S
CAS 938069-71-7
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility DMSO: 16 mg/mL(51.43 mM) DMF: 16 mg/mL(51.43 mM) Ethanol: 1 mg/ml(3.21 mM)
References 1. Guerrero, M.D., Aquino, M., Bruno, I., et al. Synthesis and pharmacological evaluation of a selected library of new potential anti-inflammatory agents bearing the γ-hydroxybutenolide scaffold: a new class of inhibitors of prostanoid production through the selective modulation of microsomal prostaglandin E synthase-1 expression. Journal of Medicinal Chemistry 50, 2176-2184 (2007). 2. Kim SH, Hashimoto Y, Cho SN, Roszik J, Milton DR, Dal F, Kim SF, Menter DG, Yang P, Ekmekcioglu S, Grimm EA. Microsomal PGE2 synthase-1 regulates melanoma cell survival and associates with melanoma disease progression. Pigment Cell Melanoma Res. 2016 May;29(3):297-308. 3. Jongthawin J, Chusorn P, Techasen A, Loilome W, Boonmars T, Thanan R, Puapairoj A, Khuntikeo N, Tassaneeyakul W, Yongvanit P, Namwat N. PGE2 signaling and its biosynthesis-related enzymes in cholangiocarcinoma progression. Tumour Biol. 2014 Aug;35(8):8051-64. 4. Xu LW, Qian M, Jia RP, Xu Z, Wu JP, Li WC, Huang WB, Chen XG. Expression and significance of microsomal prostaglandin synthase-1 (mPGES-1) and Beclin-1 in the development of prostate cancer. Asian Pac J Cancer Prev. 2012;13(4):1639-44.