Decitabine (NSC127716, 5AZA-CdR),2353-33-5,IC-0212999

Decitabine(DAC) is a deoxycytidine analogue antimetabolite with oral bioactivity and functions as an inhibitor of DNA methyltransferase. By substituting for cytosine within DNA, Decitabine covalently captures DNA methyltransferases within the DNA structure, thereby inducing irreversible inhibition of this enzyme. Decitabine has been shown to be effective against multiple cancers, including chronic myelomonocytic leukaemia (CMML), acute myeloid leukaemia (AML) [1-3].

Decitabine (10 µM; 0-120hs) treatment significantly inhibited cell growth[4]. Decitabine-pretreated(low-dose:10 nM decitabine; 24h) CD8+ T cells have increased cytotoxicity against tumors following anti-PD-1 treatment[5]. Low-dose decitabine promoted the generation of Myeloid-derived suppressor cells (MDSCs) and enhanced their aerobic metabolism and immunosuppressive functions[6]. Decitabine treatment resulted in an increased CD4:CD8 T-cell ratio and an elevation in the central memory (Tcm, CD45RO + CD62L+) and CD25-positive populations among cultured CAR T cells when compared to CAR T cells[7].

Decitabine (1.0 mg/kg; i.p.; 5days) treatment inhibits tumorigenesis and leads to regression of established tumors in mice[8]. Decitabine (1.0 mg/kg, p.o) in combination with Tetrahydrouridine (THU) causes severe toxicity in female CD-1 mice, along with an elevated sensitivity to Decitabine toxicity correlated with Decitabine plasma levels [9].