TC-E 5003

• 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[1][2][3][4].

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  AP-1; Histone Methyltransferase; NF-κB; PKA

• Type :

  Reference compound

• Related Pathways :

  Epigenetics; Immunology/Inflammation; NF-κB; Stem Cell/Wnt; TGF-beta/Smad

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Cancer; Metabolic Disease; Inflammation/Immunology

• Assay Protocol :

  https://www.medchemexpress.com/tc-e-5003.html

• Concentration :

  10mM

• Purity :

  98.03

• Solubility :

  DMSO : 125 mg/mL (ultrasonic)

• Smiles :

  O=S(C1=CC=C(NC(CCl)=O)C=C1)(C2=CC=C(NC(CCl)=O)C=C2)=O

• Molecular Formula :

  C16H14Cl2N2O4S

• Molecular Weight :

  401.26

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  PRMT1

• CAS Number :

  [17328-16-4]