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 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 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 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 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 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).
Related DNA Methyltransferase Products |
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(S)-GSK-3685032
(S)-GSK-3685032 is the inactive isomer of GSK-3685032.GSK-3685032 is a non-time-dependent, non-covalent, first-in-class, reversible selective inhibitor of DNMT1 with an IC50 value of 0.036 μM.GSK-3685032 induces DNA GSK-3685032 induces loss of DNA methylation, transcriptional activation and cancer cell growth inhibition. |
(R)-GSK-3685032
(R)-GSK-3685032 is the R-isomer of GSK-3685032.GSK-3685032 is a non-time-dependent, non-covalent, first-in-class, reversible selective inhibitor of DNMT1 with an IC50 value of 0.036 μM.GSK-3685032 induces DNA GSK-3685032 induces loss of DNA methylation, transcriptional activation and cancer cell growth inhibition. |
DNMT-IN-1
DNMT-IN-1 is a potent DNMT inhibitor with an EC50 value of 3.2 µM. |
DNMT2-IN-1
DNMT2-IN-1 is a potent and selective DNMT2 (DNA methyltransferase 2) inhibitor with an IC50 value of 1.2 μM, and has the potential for mental and metabolic disorders or cancer research. |
Guadecitabine
Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS). |
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