5-Azacytidine

Short Summary : DNA methyltransferase inhibitor.

Category : Chromatin/Epigenetics|DNA Methyltransferase

Purity : 0.9863

CAS Number : 320-67-2

Formula : C8H12N4O5

Molecular Weight : 244.2

SMILE : C1=NC(=NC(=O)N1C2C(C(C(O2)CO)O)O)N

Solubility : >12.2mg/mL in DMSO

Storage : Store at -20°C

Description : 5-Azacytidine (also known as 5-AzaC), a compound belonging to a class of cytosine analogues, is a DNA methyl transferase (DNMT) inhibitor that exerts potent cytotoxicity against multiple myeloma (MM) cells, including MM.1S, MM.1R, RPMI-8266, RPMI-LR5, RPMI-Dox40 and Patient-derived MM, with the half maximal inhibition concentration IC50 values of 1.5 mol/L, 0.7 mol/L, 1.1 mol/L, 2.5 mol/L, 3.2 mol/L and 1.5 mol/L respectively [1]. 5-Azacytidine incorporates into cellular DNA and/or RNA, subsequently sequesters DNMT and forms a covalent bond between C6 of 5-Azacytidine and cysteine thiolate of DNMTs resulting in depletion of DNMT activity in cells and demethylation of cellular DNA [1].References:[1] Kiziltepe T, Hideshima T, Catley L, Raje N, Yasui H, Shiraishi N, Okawa Y, Ikeda H, Vallet S, Pozzi S, Ishitsuka K, Ocio EM, Chauhan D, Anderson KC. 5-Azacytidine, a DNA methyltransferase inhibitor, induces ATR-mediated DNA double-strand break responses, apoptosis, and synergistic cytotoxicity with doxorubicin and bortezomib against multiple myeloma cells. Mol Cancer Ther. 2007 Jun;6(6):1718-27.

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