Drug intelligence / Profile preview

SGC707

Development stage
Preclinical
Lead developer
Structural Genomics Consortium
Modality
Small Molecules
Administration
Intraperitoneal (preclinical Studies), Potential For Oral Or Parenteral (not Clinically Established)
01

Overview

SGC707 is a potent, selective, and cell-permeable small molecule **allosteric inhibitor** of **protein arginine methyltransferase 3 (PRMT3)**, developed as a chemical probe for epigenetic research and disease modulation. SGC707 inhibits PRMT3 by targeting its dimerization interface without directly binding to the substrate or cofactor active sites. PRMT3 is a type I arginine methyltransferase involved in ribosomal biosynthesis and has been linked to cancer development and metabolic diseases. SGC707 has demonstrated the ability to reduce hepatic steatosis, lower plasma triglyceride levels, and alter lipid and bile acid metabolism in animal models. It has also shown antitumor activity in preclinical models, including effects like inhibiting cancer cell proliferation and potentiating ferroptosis in tumor cells. SGC707 is selective for PRMT3 over other methyltransferases and has excellent selectivity across a wide panel of epigenetic and non-epigenetic targets[1][3][9][11][12].

Other names
1-Isoquinolin-6-yl-3-(2-oxo-2-pyrrolidin-1-yl-ethyl)-urea
02

Targets

PRMT3 (Protein arginine N-methyltransferase 3)

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