260921
DNA Methyltransferase Inhibitor II, SGI-1027
Synonym(s):
DNA Methyltransferase Inhibitor II, SGI-1027, N-(4-(2-Amino-6-methylpyrimidin-4-ylamino)phenyl)-4-(quinolin-4-ylamino)-benzamide, S-1027, DNA MTase Inhibitor II
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About This Item
Empirical Formula (Hill Notation):
C27H23N7O
Molecular Weight:
461.52
UNSPSC Code:
12352200
Assay:
≥88% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
assay
≥88% (HPLC)
Quality Segment
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
A cell-permeable quinoline compound that is shown to inhibit human DNMT1 (IC50 = 6 and 12.5 µM, respectively, with Hemimethylated DNA or Poly(dI-dC) as the substrate), murine DNMT3a & 3b (IC50 = 8 and 7.5 µM, respectively, with Poly(dI-dC) as the substrate), as well as CpG DNA methylase M.SssI (IC50 = 13.5 and 16 µM, respectively, with Poly(dI-dC) as the substrate and 75 or 150 nM AdoMet) of mycoplasma Spiroplasma sp. strain MQ1, presumably by competing with AdoMet (S-adenosyl-L-methionine , SAM) for the enzyme′s cofactor binding site. Shown to be 2-, 3-, and 5-fold more effective than Decitabine (Cat. No. 189825), respectively, in reactivating p16 mRNA (2.5 µM for 7 days), MLH1 mRNA (2.5 µM for 7 days), and p16 protein expression (1.0 or 2.5 µM for 12 days) in human colon carcinoma RKO cultures by reducing CpG island hypermethylation found in the promoter regions of TSGs (tumor suppressor genes) without inducing genome-wide hypomethylation or caspase-3 activation.
Packaging
Packaged under inert gas
Other Notes
Datta, J., et al. 2009. Cancer Res.69, 4277.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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