SGI-1027

SGI-1027 is a quinoline-based, non-nucleoside small molecule inhibitor of DNA methyltransferases (DNMTs), specifically targeting DNMT1, DNMT3A, and DNMT3B. Developed by SuperGen (now Astex Pharmaceuticals), SGI-1027 functions as a competitive inhibitor of S-adenosyl-L-methionine (SAM), the methyl donor for DNMTs. By blocking the catalytic activity and inducing the degradation of these enzymes, the compound facilitates the reactivation of silenced tumor suppressor genes without requiring incorporation into the DNA strand, a key distinction from nucleoside analogs like decitabine. While primarily used as a potent research tool to study epigenetic regulation, preclinical studies have explored its efficacy in various cancers, including hepatocellular carcinoma and leukemia, where it demonstrates the ability to inhibit cell proliferation and induce apoptosis.

Other names

N-(4-(2-amino-6-methylpyrimidin-4-ylamino)phenyl)-4-(quinolin-4-ylamino)benzamide