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Merck
CN

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

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About This Item

Empirical Formula (Hill Notation):
C19H14N2O4
CAS Number:
Molecular Weight:
334.33
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.54
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

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

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)


Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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