Biological Activity

Decitabine is a potent DNA methyltransferase inhibitor with IC50 of 438 nM and 4.38 nM in HL-60 and KG1a cells, respectively. Decitabine is a hypomethylating agent. It hypomethylates DNA by inhibiting DNA methyltransferase. The DNA methyltransferase inhibitor Decitabine is able to reactivate genes silenced by DNA methylation and has been shown to be a very potent epigenetic compound in several hematological malignancies. Decitabine exhibits high antineoplastic activity against anaplastic large cell lymphoma (ALCL), a rare CD30 positive non-Hodgkin lymphoma of T-cell origin. The combination of Decitabine with TSA or depsi produced a greater inhibition of growth and DNA synthesis and a greater loss of clonogenicity than either agent alone. Decitabine is highly efficient against ALCL and warrants further clinical evaluation for future therapeutic use. In clinical trials, Decitabine was demonstrated to be an active antileukemic agent.

Product Citations

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  iScience. 2025 Jun 18; .

  BRAFV600E maintains the CpG island methylator phenotype and DNA methylation of PRC2 target genes in colon cancer
  Decitabine purchased from AbMole

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  iScience. 2025 May 20; .

  BRAFV600E augments WNT signalling in colorectal cancer via aberrant DNA methylation
  Decitabine purchased from AbMole

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  Patent. WO2025229179A1 2025 Nov 06; .

  Patent. WO2025229179A1
  Decitabine purchased from AbMole

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  Free Radic Biol Med. 2023 Feb 1;195:359-370.

  ROS induced the Rab26 promoter hypermethylation to promote cigarette smoking-induced airway epithelial inflammation of COPD through activation of MAPK
  Decitabine purchased from AbMole

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  Cell Biol Toxicol. 2022 Apr;38(2):291-310.

  Lnc-HZ08 regulates BPDE-induced trophoblast cell dysfunctions by promoting PI3K ubiquitin degradation and is associated with miscarriage
  Decitabine purchased from AbMole

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  Clin Epigenetics. 2021 Jul 22;13(1):142.

  Genome-wide DNA methylome analysis identifies methylation signatures associated with survival and drug resistance of ovarian cancers
  Decitabine purchased from AbMole

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  Nat Commun. 2019 Dec 20;10(1):5799.

  Novel approach reveals genomic landscapes of single-strand DNA breaks with nucleotide resolution in human cells.
  Decitabine purchased from AbMole

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  Cell Physiol Biochem. 2018;50(6):2341-2364.

  Peperomin E Induces Promoter Hypomethylation of Metastatic-Suppressor Genes and Attenuates Metastasis in Poorly Differentiated Gastric Cancer.
  Decitabine purchased from AbMole

Chemical Information

Molecular Weight	228.21
Formula	C8H12N4O4
CAS Number	2353-33-5
Solubility (25°C)	DMSO 30 mg/mL Water ≥10 mg/mL
Storage	-20°C, protect from light, sealed

References

[1] Pramod Terse, et al. Int J Toxicol. Subchronic oral toxicity study of decitabine in combination with tetrahydrouridine in CD-1 mice

[2] Li-Xin Wang, et al. PLoS One. Low dose decitabine treatment induces CD80 expression in cancer cells and stimulates tumor specific cytotoxic T lymphocyte responses

[3] Hassler MR, et al. Biochimie. Antineoplastic activity of the DNA methyltransferase inhibitor 5-aza-2'-deoxycytidine in anaplastic large cell lymphoma.

[4] Momparler RL. Semin Hematol. Pharmacology of 5-Aza-2'-deoxycytidine (decitabine).