sgc2085-hcl

Description: SGC2085 HCl, identified from virtual screening approaches, is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. Protein arginine methyltransferases (PRMTs) represent an emerging target class in oncology and other disease areas. So far, the most successful strategy to identify PRMT inhibitors has been to screen large to medium-size chemical libraries. Attempts to develop PRMT inhibitors using receptor-based computational methods have met limited success. SGC2085 which features a methyl at position R1 and a 3, 5-dimethylphenoxy at R2 has an IC50 of 50 nM for CARM1 and is over 100-fold selective for CARM1 over PRMT6. These results indicate that the presence of a substituent at R1 is essential for potent and selective inhibition of CARM1. With the exception of PRMT6 (IC50=5.2 uM), SGC2085 does not inhibit other PRMTs.

References: J Med Chem. 2016 Jul 28; 59(14):6838-47.

Related CAS#: 1821908-48-8 (free); 1821908-49-9 (HCl)