纯度:98% by TLC;NMR (Conforms)
分子式:C27H23N7O
分子量:451.52
溶剂:DMSO (35 mg/ml)
性状:Off-white solid
存储:-20°C
Activity (short version):DNA methyl transferase inhibitor
Function / Pharmacology:Potent and selective inhibitor of DNA methyl transferase inhibiting DNMT1, DNMT3A and DNMT3B with comparable potency (IC50=12.5, 8.0 and 7.5 ?M respectively).1 Treatment of various cancer cell lines with SGI-1027 results in selective degradation of DNMT1 (MG-132 sensitive) with minimal effect on DNMT3A and 3B at 2.5-5 ?M.1 Prolonged treatment of RKO cells resulted in reexpression of silenced tumor suppressor genes.1 Synergizes with doxorubicin at growth inhibition in neuroblastoma cell lines.2 Disrupts the MKK3-MYC complex in cells and inhibits MYC transcriptional activity in colon and breast cancer cells.3