5-Azacytidine

5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes^[1][2]. 5-Azacytidine induces cell autophagy^[4]. IC50 & Target:IC50: DNA methyltransferases; autophagy^[1] In Vitro: Unmethylated CpG islands associated with a variety of genes become partially or fully methylated in tumors and can be reactivated by 5-Azacytidine^[1]. 5-Azacytidine acts as weak inducers of erythroid differentiation of Friend erythroleukemia cells in the same concentration range where they affect DNA methyltransferase activity^[2]. 5-Azacytidine inhibits L1210 cells with ID₅₀ and ID₉₀ values of 0.019 and circa 0.15 μg/mL, respectively^[3]. In Vivo: TdR-³H incorporation is significantly inhibited when the animals are exposed to 5-Azacitidine (100 mg/kg, i.p.) for 2 hr or longer^[3].