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.
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 (5-Aza-2'-deoxycytidine) purchased from AbMole
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 (5-Aza-2'-deoxycytidine) purchased from AbMole
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 (5-Aza-2'-deoxycytidine) purchased from AbMole
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 (5-Aza-2'-deoxycytidine) purchased from AbMole
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 (5-Aza-2'-deoxycytidine) purchased from AbMole
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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Momparler RL. Semin Hematol. Pharmacology of 5-Aza-2'-deoxycytidine (decitabine).
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Procainamide
Procainamide is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1). Procainamide is a Class 1A antiarrhythmic agent. Procainamide has the potential for the research of cancer and arrhythmias. |
GSK-3484862
GSK-3484862 is a non-covalent inhibitor for Dnmt1. GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates global demethylation in murine embryonic stem cells. |
O6BTG-octylglucoside
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Bobcat339 hydrochloride
Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. |
5-Methyl-2'-deoxycytidine
5-Methyl-2'-deoxycytidine in single-stranded DNA can act in cis to signal de novo DNA methylation. |
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