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TC-E 5003 is a selective inhibitor of PRMT1 with IC50 value of 1.5 μM [1].

PRMT1 is a member of the protein arginine N-methyltransferase (PRMT) family and plays a pivotal role in many biological processes by post-translational modification of target proteins. It has been reported that PRMT1 abnormal expression was observed in many types of cancer and its inhibitors was regarded as promising target in clinic [2].

TC-E 5003 is a potent PRMT1 inhibitor. When tested with breast cancer cell line MCF7a or prostate cancer cell line LNCaP, TC-E treatment induced cell apoptosis and inhibited cell proliferation by functioning on PRMT1. And it also reported that TC-E treatment attenuated androgen-induced gene expression in LNCaP cells [1].

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