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]. In Vitro:TC-E 5003 (0-1 μM, 24 h) suppresses LPS-induced NO production in RAW264.7 cells^[1].
TC-E 5003 (1 μM, 15-60 min) regulates LPS-induced AP-1 transcriptional activity by modulating the c-Jun gene expression in RAW264.7 cells^[1].
TC-E 5003 (10 μM, 4 h) augments thermogenesis through increase in UCP1 expression without changing mitochondrial content and activates the downstream molecules of PKA signaling in primary iWAT cells^[2].
TC-E 5003 (6 μM, 48 h) has a good inhibition on the proliferation of cancer cells^[3].
In Vivo:TC-E 5003 (0.5-2.0 mg, s.c., a single dose for 28 days) has an excellent tumor-suppressing effect in A549 tumor xenograft ICR mouse models ^[3].