tcsc2735 SGI-1027

SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC₅₀s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.

IC50 & Target: IC50: 7.5 μM (DNMT3B), 8 μM (DNMT3A), 12.5 μM (DNMT1)^[1]

In Vitro: SGI-1027 is a DNMT inhibitor, with IC₅₀s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate. SGI-1027 shows an IC₅₀ of 6 μM for DNMT1 (hemimethylated DNA). SGI-1027 (1, 2.5, or 5 µM) causes selective degradation of DNMT1 in several human cancer cell lines, but shows little or no cytotoxic effect on rat hepatoma cells, and does not induce apoptosis in rat hepatoma cells^[1]. SGI-1027 shows an EC₅₀ of 0.9 μM for hDNMT3A, and causes cytotoxicity on KG-1 cells, with an EC₅₀ of 4.4 μM^[2].