CAY10723 (hydrochloride)

CAY10723 is an inhibitor of peptidyl arginine deiminase 2 (PAD2; EC50 = 9.5 μM in a cellular target engagement assay).1 It is approximately 1.6-, 47-, and 15-fold selective for PAD2 over PAD1, PAD3, and PAD4, respectively. CAY10723 inhibits histone H3 citrullination in HEK293T cells expressing human PAD2 (EC50 = 0.4 μM). It also inhibits fibrinogen citrullination in the presence of isolated human polymorphonuclear leukocytes (PMNs) or synovial fluid from patients with rheumatoid arthritis when used at a concentration of 20 µM.2 CAY10723 (25 µM) decreases IFN-γ production in isolated human CD4+ T cells.3WARNING This product is not for human or veterinary use.

[1] AARON MUTH. Development of a Selective Inhibitor of Protein Arginine Deiminase 2[J]. Journal of Medicinal Chemistry, 2017, 60 7: 3198-3211. DOI: 10.1021/acs.jmedchem.7b00274
[2] MARÍA TERESA MARTÍN MONREAL. Applicability of Small-Molecule Inhibitors in the Study of Peptidyl Arginine Deiminase 2 (PAD2) and PAD4.[J]. Frontiers in Immunology, 2021: 716250. DOI: 10.3389/fimmu.2021.716250
[3] YUDONG LIU. Peptidylarginine deiminases 2 and 4 modulate innate and adaptive immune responses in TLR-7-dependent lupus.[J]. JCI insight, 2018, 3 23. DOI: 10.1172/jci.insight.124729
[4] SELINA PASQUERO . Novel antiviral activity of PAD inhibitors against human beta-coronaviruses HCoV-OC43 and SARS-CoV-2[J]. Antiviral research, 2022, 200: Article 105278. DOI: 10.1016/j.antiviral.2022.105278