260920

DNA Methyltransferase Inhibitor

The DNA Methyltransferase Inhibitor, also referenced under CAS 32675-71-1, controls the biological activity of DNA Methyltransferase. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Synonym(s): DNA Methyltransferase Inhibitor, 2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-(1H-indol-3-yl)propionic acid, RG108, DNA MTase Inhibitor I
• Empirical Formula (Hill Notation): C₁₉H₁₄N₂O₄
• CAS Number: 32675-71-1
• Molecular Weight: 334.33
• UNSPSC Code: 12352200

Properties

• Quality Level: 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
• 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

Description

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable