AM9053

AM9053 is a selective, effective and slowly reversible inhibitor of N-acyl ethanolamine acid amidease ( NAAA ) ( IC₅₀ = 30 nM). The effect of AM9053 on FAAH activity is limited ( IC₅₀ > 100 nM). AM9053 inhibits the proliferation of colorectal cancer cells by activating the PPAR-α and TRPV1 dependent mechanisms and induces S-phase cell cycle arrest. AM9053 alleviates intestinal fibrosis by regulating macrophage activity and inhibiting the IL-23 signaling pathway. AM9053 leads to an increase in NAE levels, especially PEA and OEA. AM9053 can be used for the study of colorectal cancer and intestinal fibrosis ^{[1] [2] [3]}.

References:
[1]. Bottemanne P, et al. N-acylethanolamine hydrolyzing acid amidase inhibition: tools and potential therapeutic opportunities. Drug Discov Today. 2018 Aug;23(8):1520-1529.
[2]. Nanì MF, et al. Pharmacological Inhibition of N-Acylethanolamine Acid Amidase (NAAA) Mitigates Intestinal Fibrosis Through Modulation of Macrophage Activity. J Crohns Colitis. 2025 Feb 4;19(2):jjae132.
[3]. Romano B, et al. N-Acylethanolamine acid amidase (NAAA) is dysregulated in colorectal cancer patients and its inhibition reduces experimental cancer growth. Br J Pharmacol. 2022 Apr;179(8):1679-1694.