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MedChemExpress - Model TC-E 5003 - ...

MedChemExpress - Model TC-E 5003 - 17328-16-4

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].

TC-E 5003

MCE China：TC-E 5003

Brand：MedChemExpress (MCE)

Cat. No.HY-107574

CAS：17328-16-4

Purity：98.03%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

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].

IC50 & Target：PRMT1

References：

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[4]. Shen NY, et al. Protein arginine methyltransferase expression and activity during myogenesis. Biosci Rep. 2018 Jan 10;38(1):BSR20171533. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。