TC-E 5003

TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers[1][2][3][4].

[1]Kim E, et al. Protein Arginine Methyltransferase 1 (PRMT1) Selective Inhibitor, TC-E 5003, Has Anti-Inflammatory Properties in TLR4 Signaling. Int J Mol Sci. 2020;21(9):3058. Published 2020 Apr 26. |[2]Park MJ, et al. TC-E 5003, a protein methyltransferase 1 inhibitor, activates the PKA-dependent thermogenic pathway in primary murine and human subcutaneous adipocytes. FEBS Lett. 2020 Sep;594(17):2923-2930.|[3]Zhang P, et al. Developing protein arginine methyltransferase 1 (PRMT1) inhibitor TC-E-5003 as an antitumor drug using INEI drug delivery systems. Drug Deliv. 2020 Dec;27(1):491-501.|[4]Shen NY, et al. Protein arginine methyltransferase expression and activity during myogenesis. Biosci Rep. 2018 Jan 10;38(1):BSR20171533.