RG108---DNA Methyltransferase Inhibitor

RG108 is a non-nucleoside DNA methyltransferase inhibitor (DNMT inhibitor). RG108 led to a significant dose and time dependent growth inhibition and apoptosis induction in LNCaP, 22Rv1 and DU145. LNCaP and 22Rv1 also displayed decreased DNMT activity, DNMT1 expression and global DNA methylation. Interestingly, chronic treatment with RG108 significantly decreased GSTP1, APC and RAR-β2 promoter hypermethylation levels, although mRNA reexpression was only attained for GSTP1 and APC. RG108 is an effective tumor growth suppressor in most PCa cell lines tested.

Product information

CAS Number: 48208-26-0

Molecular Weight: 334.33

Formula: C19H14N2O4

Chemical Name: (S)-2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl)propanoic acid

Smiles: OC(=O)[C@H](CC1=CNC2=CC=CC=C21)N1C(=O)C2=CC=CC=C2C1=O

InChiKey: HPTXLHAHLXOAKV-INIZCTEOSA-N

InChi: 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)/t16-/m0/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

RG108 was used at 10-100 µM final concentration in various in vitro assays.

References:

1. Brueckner B, et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. (2005) Cancer Res. 65(14):6305-11.
2. Stresemann C, et al. Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. (2006) Cancer Res. 66(5):2794-800.
3. Schirrmacher E, et al. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. (2006) Bioconjug Chem. 17(2):261-6.
4. Shi Y, et al. Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. (2008) Cell Stem Cell. 3(5):568-74.
5. Pasha Z, et al. Efficient non-viral reprogramming of myoblasts to stemness with a single small molecule to generate cardiac progenitor cells. (2011) PLoS One. 6(8):e23667.

Products are for research use only. Not for human use.