TC-E 5003

TC-E 5003 is a **selective small molecule inhibitor of protein arginine N-methyltransferase 1 (PRMT1)**, with an IC50 value of approximately 1.5 μM. PRMT1 is the predominant type I PRMT, catalyzing asymmetric dimethylation of arginine residues on histones and other proteins—an epigenetic modification critical in transcriptional regulation and oncogenic transformation. TC-E 5003 shows no significant activity against CARM1 or Set7/9 methyltransferases. In preclinical studies, TC-E 5003 inhibited growth and induced apoptosis of MCF-7 (breast cancer) and LNCaP (prostate cancer) cells, as well as several other cancer lines (A549, H1299, MDA-MB-231)[1][2][3][5]. It also attenuates androgen-induced gene expression in prostate cancer cells. In vivo xenograft models show anti-tumor effects and low toxicity. Notably, recent research shows that in primary adipocytes, TC-E 5003 activates the PKA-dependent thermogenic pathway and induces thermogenic gene expression in a PRMT1-independent manner, suggesting other bioactive effects[9]. Primarily used in cancer research and epigenetic studies, TC-E 5003 is for research use only and not for clinical use.

Other names

N,N'-(Sulfonyldi-4,1-phenylene)bis(2-chloroacetamide)