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.
Biochem/physiol Actions
SGI-1027 is a DNA methyltransferase (DNMT) inhibitor with IC50 values of 6-13 µM for DNMT3B, DNMT3A and DNMT1. SGI-1027 directly inhibits DNMT activity by competing with the cofactor, S-adenosylmethionine (SAM) in the methylation reaction. SGI-1027 treatment of cancer cell lines induced degradation of DNMT1, but not DNMT3A or DNMT3B, and in RKO cells caused re-expression of the silenced tumor supressor genes p16, MLH1 and TIMP3.
Packaging
5, 25 mg in glass bottle
| Colour | white to light brown |
|---|---|
| Quality Level | 100 |
| InChI key | QSYLKMKIVWJAAK-UHFFFAOYSA-N |
| InChI | 1S/C27H23N7O/c1-17-16-25(34-27(28)30-17)32-20-10-12-21(13-11-20)33-26(35)18-6-8-19(9-7-18)31-24-14-15-29-23-5-3-2-4-22(23)24/h2-16H,1H3,(H,29,31)(H,33,35)(H3,2 |
| Manufacturer | SIGMA-ALDRICH |
| Solubility | DMSO: 20 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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