RG108
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MedKoo CAT#: 406615

CAS#: 48208-26-0

Description: 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.


Chemical Structure

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RG108
CAS# 48208-26-0

Theoretical Analysis

MedKoo Cat#: 406615
Name: RG108
CAS#: 48208-26-0
Chemical Formula: C19H14N2O4
Exact Mass: 334.09536
Molecular Weight: 334.32546
Elemental Analysis: C, 68.26; H, 4.22; N, 8.38; O, 19.14

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 2 Weeks
25.0mg USD 250.0 2 Weeks
50.0mg USD 450.0 2 Weeks
100.0mg USD 650.0 2 Weeks
200.0mg USD 950.0 2 Weeks
500.0mg USD 1650.0 2 Weeks
1.0g USD 2350.0 2 Weeks
2.0g USD 3950.0 2 Weeks
5.0g USD 6450.0 2 Weeks
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Synonym: RG108; RG-108; RG 108; N-Phthalyl-L-tryptophan.

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

InChi Key: HPTXLHAHLXOAKV-INIZCTEOSA-N

InChi Code: 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

SMILES Code: O=C(O)[C@H](CC1=CNC2=CC=CC=C12)N3C(C4=CC=CC=C4C3=O)=O

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 334.32546 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Asgatay S, Champion C, Marloie G, Drujon T, Senamaud-Beaufort C, Ceccaldi A, Erdmann A, Rajavelu A, Schambel P, Jeltsch A, Lequin O, Karoyan P, Arimondo PB, Guianvarc'h D. Synthesis and evaluation of analogues of N-phthaloyl-l-tryptophan

(RG108) as inhibitors of DNA methyltransferase 1. J Med Chem. 2014 Jan 23;57(2):421-34. doi: 10.1021/jm401419p. Epub 2014 Jan 9. PubMed PMID: 24328113.

2: Graça I, Sousa EJ, Baptista T, Almeida M, Ramalho-Carvalho J, Palmeira C, Henrique R, Jerónimo C. Anti-tumoral effect of the non-nucleoside DNMT inhibitor RG108 in human prostate cancer cells. Curr Pharm Des. 2014;20(11):1803-11. PubMed PMID: 23888969.

3: Savickiene J, Treigyte G, Jazdauskaite A, Borutinskaite VV, Navakauskiene R. DNA methyltransferase inhibitor RG108 and histone deacetylase inhibitors cooperate to enhance NB4 cell differentiation and E-cadherin re-expression by chromatin remodelling. Cell Biol Int. 2012 Nov 1;36(11):1067-78. doi: 10.1042/CBI20110649. PubMed PMID: 22845560.

4: Savickiene J, Treigyte G, Borutinskaite VV, Navakauskiene R. Antileukemic activity of combined epigenetic agents, DNMT inhibitors zebularine and RG108 with HDAC inhibitors, against promyelocytic leukemia HL-60 cells. Cell Mol Biol Lett. 2012 Dec;17(4):501-25. Epub 2012 Jul 20. PubMed PMID: 22820861.

5: Braun J, Boittiaux I, Tilborg A, Lambert D, Wouters J. The dicyclo-hexyl-amine salt of RG108 (N-phthalyl-l-tryptophan), a potential epigenetic modulator. Acta Crystallogr Sect E Struct Rep Online. 2010 Nov 13;66(Pt 12):o3175-6. doi: 10.1107/S160053681004626X. PubMed PMID: 21589471; PubMed Central PMCID: PMC3011641.

6: Schirrmacher E, Beck C, Brueckner B, Schmitges F, Siedlecki P, Bartenstein P, Lyko F, Schirrmacher R. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug Chem. 2006 Mar-Apr;17(2):261-6. PubMed PMID: 16536454.

RG108

10.0mg / USD 150.0


Additional Information