1. Epigenetics
  2. DNA Methyltransferase
  3. 5-Aza-4'-thio-2'-deoxycytidine

5-Aza-4'-thio-2'-deoxycytidine (Synonyms: 5-Aza-T-dCyd)

Cat. No.: HY-139015
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5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects.

For research use only. We do not sell to patients.

5-Aza-4'-thio-2'-deoxycytidine Chemical Structure

5-Aza-4'-thio-2'-deoxycytidine Chemical Structure

CAS No. : 169514-76-5

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Description

5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects[1].

IC50 & Target[1]

DNMT1

 

In Vitro

5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd; 72 h) inhibits leukemia lines: CCRF-CEM (IC50=0.2 μM), KG1a (IC50=0.06 μM). 5-Aza-4'-thio-2'-deoxycytidine also decreases viability in the NCI-H23 lung carcinoma (IC50=4.5 μM), HCT-116 colon carcinoma (IC50=58 μM) and IGROV-1 ovarian carcinoma (IC50=36 μM)[1].
5-Aza-4'-thio-2'-deoxycytidine (0.1-20 μM; 96 h) markedly depletes DNMT1 in NCI-H23 lung, HCT-116 colon and IGROV-1 ovarian cells. 5-Aza-4'-thio-2'-deoxycytidine (0.1, 0.5, 1 μM; 96 h) results in marked depletion of DNMT1 in CCRF-CEM and KG1a myeloid leukemia cells[1].
5-Aza-4'-thio-2'-deoxycytidine (1 μM; 96 h) induce CpG demethylation and re-expression of the p15 tumor suppressor gene[1].

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

Western Blot Analysis[1]

Cell Line: NCI-H23 lung, HCT-116 colon and IGROV-1 ovarian cells
Concentration: 1, 5, 10, 20 μM
Incubation Time: 96 h
Result: Markedly depleted DNMT1 in cells.
In Vivo

5-Aza-4'-thio-2'-deoxycytidine (6.7, 10 mg/kg/day; IP; for 9 days) is effective against NCI-H23 tumor xenografts[1].
5-Aza-4'-thio-2'-deoxycytidine (5 mg/kg/day; IP; for 9 days) decreases DNMT1 levels in tumors of CCRF-CEM tumors mice xenografts[1].
5-Aza-4'-thio-2'-deoxycytidine (1.5 mg/kg; ip; QD×5 rest and repeat 3 cycles) provides modest suppression of tumor growth as well in the HCT116 colon carcinoma, OVCAR3 ovarian tumor xenograft model. 5-Aza-4'-thio-2'-deoxycytidine has minimal antitumor effect in the HL-60 leukemia xenografts[2].

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

Animal Model: Young female athymic nu/nu mice with NCI-H23 tumor fragment[1]
Dosage: 6.7 or 10 mg/kg
Administration: IP; daily for 9 days
Result: Had antitumor efficacy against NCI-H23 tumor xenografts.
Molecular Weight

244.27

Formula

C₈H₁₂N₄O₃S

CAS No.
SMILES

O=C1N(C=NC(N)=N1)[[email protected]]2([H])S[[email protected]@H]([[email protected]](C2)O)CO

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

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Keywords:

5-Aza-4'-thio-2'-deoxycytidine5-Aza-T-dCydDNA MethyltransferaseDNMTsDNA MTasesorallyhypomethylatingleukemiaCCRF-CEMKG1aNCI-H23HCT-116IGROV-1Inhibitorinhibitorinhibit

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5-Aza-4'-thio-2'-deoxycytidine
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HY-139015
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