5-Azacytidine --- DNA Methyltransferase Inhibitor

5-Azacytidine is a classic DNA methyltransferase inhibitor. It incorporates into DNA forming covalent adducts with cellular DNMT, depleting enzyme activity. Azacitidine is widely used to demonstrate the correlation between loss of methylation in specific gene regions and activation of the associated genes. It can also improve the efficiency of reprogramming of stem cells, induce differentiation of mesenchymal stem cells into cardiomyocytes.

Product information

CAS Number: 320-67-2

Molecular Weight: 244.20

Formula: C8H12N4O5

Synonym:

5-AZAC

Azacitidine

Azacytidine

Mylosar

Vidaza

Azacitidinum

Azacitidina

4-Amino-1-beta-D-ribofuranosyl-s-triazin-2(1H)-one

5-AZCR

5 AZC

MFCD00006539

Chemical Name: 4-amino-1-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1,3,5-triazin-2(1H)-one

Smiles: NC1=NC(=O)N(C=N1)[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O

InChiKey: NMUSYJAQQFHJEW-KVTDHHQDSA-N

InChi: InChI=1S/C8H12N4O5/c9-7-10-2-12(8(16)11-7)6-5(15)4(14)3(1-13)17-6/h2-6,13-15H,1H2,(H2,9,11,16)/t3-,4-,5-,6-/m1/s1

Technical Data

Appearance: White Solid Powder

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: H2O : 33.33 mg/mL (136.49 mM; Need ultrasonic); DMSO : ≥ 31 mg/mL (126.95 mM)

Shipping Condition: Room temperature in continental US; may vary elsewhere.

Storage Condition: Powder: 4^oC 1 year, -20^oC 3 years

Shelf Life: ≥36 months if stored properly.

Stock Solution Storage: DMSO: 4^oC 3 month.

Drug Formulation: This drug may be formulated in DMSO

HS Tariff Code: 2934.99.9001

How to use

In Vitro:

5-Azacytidine was used at 3-10µM final concentration in various in vitro assays.

In Vivo:

5-Azacytidine was intraperitoneally (IP) dosed to mice at 3 mg/kg once per day. It is dissolved in 0.85% NaCl solution immediately prior to use.

References:

1. Qian Q, et al. 5-Azacytidine induces cardiac differentiation of human umbilical cord-derived mesenchymal stem cells by activating extracellular regulated kinase. (2012) Stem Cells Dev. 21(1):67-75.
2. Mikkelsen TS, et al. Dissecting direct reprogramming through integrative genomic analysis. (2008) Nature. 454(7200):49-55.
3. Schneider-Stock R, et al. 5-Aza-cytidine is a potent inhibitor of DNA methyltransferase 3a and induces apoptosis in HCT-116 colon cancer cells via Gadd45- and p53-dependent mechanisms. (2005) J Pharmacol Exp Ther. 312(2):525-36.
4. Christman JK, et al. 5-Azacytidine and 5-aza-2'-deoxycytidine as inhibitors of DNA methylation: mechanistic studies and their implications for cancer therapy. (2002) Oncogene. 21(35):5483-95.

Products are for research use only. Not for human use.

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