Decitabine methanesulfonate (Synonyms: 5-Aza-2'-deoxycytidine methanesulfonate; 5-AZA-CdR methanesulfonate; NSC 127716 methanesulfonate)

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Decitabine methanesulfonate (5-Aza-2'-deoxycytidine methanesulfonate) is an orally active Deoxycytidine analogue antimetabolite and DNA methyltransferase inhibitor. Decitabine methanesulfonate incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine methanesulfonate induces cell G2/M arrest and cell Apoptosis. Decitabine has potent anticancer activity.

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CAS No. : 879492-57-6

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Other In-stock Forms of Decitabine methanesulfonate:

Decitabine

Other Forms of Decitabine methanesulfonate:

Decitabine In-stock

168 Publications Citing Use of MCE Decitabine methanesulfonate

RT-PCR

Cell Proliferation/Viability Assay

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: Cell. 2024 Apr 25;187(9):2288-2304.e27. [Abstract]; SLC6A6 mRNA levels in the indicated cells treated with decitabine (1 μM for 3 days).

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2022 Mar 29;2022:2371807. [Abstract]; The toxicity of decitabine to Y79 and WERI-RB-1 cells is detected by CCK-8 assay at different concentrations of Decitabine.

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2022 Mar 29;2022:2371807. [Abstract]; The mRNA expression of GSDME is detected using RT-PCR after treatment with different concentrations of Decitabine for 3 days (the cells were centrifuged, and decitabine is replaced every day).

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2022 Mar 29;2022:2371807. [Abstract]; The protein level of GSDME in cells is quantitatively analysed by western blot in Y79 and WERI-RB-1 cells after Decitabine (2 nM; 3 days) treatment.

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2022 Mar 29;2022:2371807. [Abstract]; The protein level of GSDME in cells is detected using immunofluorescence in Y79 and WERI-RB-1 cells after Decitabine (2 nM; 3 days) treatment.

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: Prog Neurobiol. 2021 Jun:201:102028. [Abstract]; The TF changes induced by DNMT3L in these cells are not affected with Decitabine (10 µM; for 24 hours) treatment in most genes tested, except NEUROD2 and NEUROG2 as shown by qRTPCR.

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2021 Jul;54(7):e13072. [Abstract]; The indicated HSCs are subjected to DNMTs inhibitor (5‐azadC, 2 μM), G9a inhibitor (UNC0642, 2 μM) and pan‐HDAC inhibitor (ITF‐2357, 100 nM) for 48 h, or EZH2 inhibitor (EPZ‐6438, 10 μM) for 72h. KLF14 expression is measured by RT‐qPCR.

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2021 Jul;54(7):e13072. [Abstract]; The indicated HSCs are subjected to DNMTs inhibitor (5‐azadC, 2 μM), G9a inhibitor (UNC0642, 2 μM) and pan‐HDAC inhibitor (ITF‐2357, 100 nM) for 48 h, or EZH2 inhibitor (EPZ‐6438, 10 μM) for 72h. KLF14 expression is measured by Western blotting analyses.

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: Oncogene. 2020 Aug;39(33):5507-5519. [Abstract]; Quantitative real-time PCR analysis of CDH13 expression after 5 μM Decitabine treatment.

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: J Invest Dermatol. 2020 Dec;140(12):2442-2454.e5. [Abstract]; In EZH2 mutant cells, after six days of drug treatment with both GSK126 and 0.5 μM Decitabine, Western blots shows complete elimination of H3K37me3 with reductions in DNMT1A, DNMT3A, and DNMT3B.

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: J Invest Dermatol. 2020 Dec;140(12):2442-2454.e5. [Abstract]; In EZH2 mutant cells, after six days of drug treatment with both GSK126 and 0.5 μM Decitabine, Significant upregulation of RASSF5, EPAS1, ITGB2, and NDRG1 target gene expression is seen in EZH2 mutant cell lines.

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2019 Oct;78(10):1420-1429. [Abstract]; Western blot of PPARγ from mouse chondrocytes treated with IL-1β (10 ng/mL) for 24 hours in absence or presence 5Aza of various doses (0, 1, 5 and 10 µM).

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2019 Oct;78(10):1420-1429. [Abstract]; Western blot of PPARγ, MMP13, Aamts5, Aggrecan and Collagen2 from Sham, DMM and 5Aza-treated mouse joint tissues (0.35 mg/kg; intraperitoneal injection daily; 10 weeks).

: Decitabine methanesulfonate purchased from MedChemExpress. Usage Cited in: J Allergy Clin Immunol. 2019 Jun;143(6):2038-2051.e12. [Abstract]; Naive CD4⁺ T cells are stimulated with anti-CD3/CD28 in the presence of mock stimulant or Decitabine (5-aza-29-deoxycytidine; 1 µM). Real-time PCR analysis of Il4 and Il13 mRNA after 24 hours of stimulation and IL-4 and IL-13 concentrations in culture supernatants after 72 hours of stimulation are measured.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

Decitabine methanesulfonate (96 h) treatment significantly inhibits cell growth of SNU719, NCC24 and KATOIII 96 hours after exposure to decitabine. Decitabine methanesulfonate induces G2/M arrest and apoptosis in EBVaGC, inhibits invasion ability, and up-regulates E-cadherin expression for EBVaGC^[1].
Only high concentrations (10 μM) Decitabine (0.1-10 μM; 24-72 h) methanesulfonate results in a G2 phase arrest, which is accompanied by a reduction of cells in G1 phase in HCT116 cells^[3].
Decitabine methanesulfonate up-regulates DCTPP1 and dUTPase expression in HeLa cells^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[3]

Cell Line:	HCT116 cells
Concentration:	0.1, 1, 10 µM
Incubation Time:	24, 48, 72 hours
Result:	Only high concentrations (10 µM) resulted in a G2 phase arrest, which was accompanied by a reduction of cells in G1 phase.

In Vivo

Decitabine (1.0 mg/kg, p.o.) methanesulfonate in combination with tetrahydrouridine (THU) causes severe toxicity occurs in female CD-1 mice, and results in an increased sensitivity to decitabine toxicity correlating with decitabine plasma levels^[5].
Decitabine (1.0 mg/kg; i.p.; once daily for 5 consecutive days) methanesulfonate leads to regression of EL4 tumors established in C57BL/6 Mice^[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 mice (bearing EL4 cells)^[7]
Dosage:	1.0 mg/kg
Administration:	Intraperitoneal injection; once daily for 5 consecutive days
Result:	Caused continuous tumor regression even after Decitabine methanesulfonate treatment was stopped.

Molecular Weight

324.31

Formula

C₉H₁₆N₄O₇S

CAS No.

879492-57-6

SMILES

CS(=O)(O)=O.O=C1N(C=NC(N)=N1)[C@@H]2O[C@@H]([C@H](C2)O)CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Nakamura M, et al. Decitabine inhibits tumor cell proliferation and up-regulates E-cadherin expression in Epstein-Barr virus-associated gastric cancer. J Med Virol. 2016 Jul 19. [Content Brief]

[2]. Parker WB. Enzymology of purine and pyrimidine antimetabolites used in the treatment of cancer. Chem Rev. 2009 Jul;109(7):2880-93. [Content Brief]

[3]. Hagemann S, et al. Azacytidine and decitabine induce gene-specific and non-random DNA demethylation in human cancer cell lines. PLoS One. 2011 Mar 7;6(3):e17388. [Content Brief]

[4]. Requena CE, et al. The nucleotidohydrolases DCTPP1 and dUTPase are involved in the cellular response to decitabine. Biochem J. 2016 Jun 20. [Content Brief]

[5]. Terse P, et al. Subchronic oral toxicity study of decitabine in combination with tetrahydrouridine in CD-1 mice. Int J Toxicol. 2014 Mar-Apr;33(2):75-85. [Content Brief]

[6]. Yu J, et al. DNA methyltransferase expression in triple-negative breast cancer predicts sensitivity to decitabine. J Clin Invest. 2018 Jun 1;128(6):2376-2388. [Content Brief]

[7]. Wang LX, et al. Low dose decitabine treatment induces CD80 expression in cancer cells and stimulates tumorspecific cytotoxic T lymphocyte responses. PLoS One. 2013 May 9;8(5):e62924. [Content Brief]

Decitabine methanesulfonate Related Classifications

Cancer

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Decitabine879492-57-65-Aza-2'-deoxycytidine5-AZA-CdRNSC 127716NSC127716NSC-127716DNA MethyltransferaseApoptosisNucleoside Antimetabolite/AnalogDNMTsDNA MTasesInhibitorinhibitorinhibit

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