RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 48208-26-0
- 화학식: C19H14N2O4
- 분자량:334.33
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
[1]|
CpG methylase M.SssI 115 nM (IC50) |
In Vitro
RG108 (GMP) effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 (GMP) results in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 (GMP) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences[1].
In another study, the synthesis and in vitro analysis of a biotinylated RG108 (GMP) conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes[2].
In a recent study, it is shown RG108 (GMP) can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 48208-26-0
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분자량 334.33
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화학식 C19H14N2O4
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SMILES
O=C(N1[C@H](C(O)=O)CC2=CNC3=C2C=CC=C3)C4=CC=CC=C4C1=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Brueckner B, et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res. 2005 Jul 15;65(14):6305-11. [Content Brief]
[2]. Schirrmacher E, et al. 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. [Content Brief]
[3]. Pasha Z, et al. Efficient non-viral reprogramming of myoblasts to stemness with a single small molecule to generate cardiac progenitor cells. PLoS One. 2011;6(8):e23667. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RG108 (GMP) Related Classifications
HY-13642G Related Classifications
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