tcsc0372 Decitabine

Decitabine (NSC 127716) is a DNA methyltransferase inhibitor commonly used to treat myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML).

In Vitro: Decitabine treatment significantly inhibits cell growth of SNU719, NCC24 and KATOIII 96 hours after exposure to decitabine. Decitabine induces G2/M arrest and apoptosis in EBVaGC, inhibits invasion ability, and up-regulates E-cadherin expression for EBVaGC^[1]. Tri-acetylation on the H4 N-terminal tail (H4K8acK12acK16ac) is reduced after DAC treatment in MDS-L sensitive cells^[2]. Decitabine up-regulates DCTPP1 and dUTPase expression in HeLa cells^[3].

In Vivo: Decitabine (1.0 mg/kg, p.o.) in combination with tetrahydrouridine (THU) causes severe toxicity occurs in females, and results in an increased sensitivity to decitabine toxicity correlating with decitabine plasma levels^[4].