DNA methyltransferase inhibitor. Inhibits the mammalian DNA methyltransferases DNMT3B, DNMT3A and DNMT1 (IC50values are 7.5, 8 and 12.5μM with Poly(dl-dC) as the substrate). Reactivates silenced tumor suppressor genes by reducing CpG island hypermethylati
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of DNA methyltransferase 1
Product Description
Application:
SGI-1027 has been used as a DNA methyltransferase inhibitor to study its effects on gene expression during osteogenic differentiation. It has also been used as a DNA methyltransferase 3a inhibitor to study its effects on interleukin-6 (IL-6)-induced loss of forkhead box P3 (Foxp3) gene expression in B-lymphocyte-induced maturation protein 1 (Blimp1)-Treg cells.
1.Valente S, Liu Y, Schnekenburger M, Zwergel C, Cosconati S, Gros C, Tardugno M, Labella D, Florean C, Minden S et al.. (2014) Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.. J Med Chem, 57 (3):(701-13). [PMID:24387159][10.1021/op500134e]
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