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General description
A cell-permeable, specific DNA methyltransferases inhibitor (IC50 = 115 nM for CpG methylase M.SssI) that displays anti-proliferative, but not cytotoxic, properties. Unlike the commonly used inhibitor 5-azacytidine, RG108 directly interacts with DNA methyltransferase active site via its carboxy group.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CPG methylase M.Sssl
Product does not compete with ATP.
Reversible: no
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Brueckner, B., et al. 2005. Cancer Res.65, 6305.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | solid |
| potency | 115 nM IC50 |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | yellow |
| solubility | DMSO: 100 mg/mL,methanol: soluble |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | [nH]1c2c(c(c1)CC(N3C(=O)c4c(cccc4)C3=O)C(=O)O)cccc2 |
| InChI | 1S/C19H14N2O4/c22-17-13-6-1-2-7-14(13)18(23)21(17)16(19(24)25)9-11-10-20-15-8-4-3-5-12(11)15/h1-8,10,16,20H,9H2,(H,24,25) |
| InChI key | HPTXLHAHLXOAKV-UHFFFAOYSA-N |
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¥ 4897.21
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¥ 14407.09
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¥ 2666.57
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¥ 745.60
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¥ 1196.14
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¥ 3662.39
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¥ 39793.68
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¥ 65710.50
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¥ 42661.77
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¥ 57595.03
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