RG108-N-Phthalyl-L-tryptophan-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERG108Cat. No.: HY-13642CAS No.: 48208-26-0Synonyms: N-Phthalyl-L-tryptophan分式: CHNO分量: 334.33作靶点: DNA Methyltransferase作通路: Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg

2、/mL (299.11 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9911 mL 14.9553 mL 29.9106 mL5 mM 0.5982 mL 2.9911 mL 5.9821 mL10 mM 0.2991 mL 1.4955 mL 2.9911 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现

3、现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.48 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.48 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master o

4、f Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (7.48 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 RG108种核苷的 DNA 甲基转移酶 (DNA methyltransferase) 抑制剂，IC50 值为 115 nM。IC50 & Target CpG methylase M.SssI115 nM (IC50)体外研究 RG108 effectively blocks DNA methyltransferases in vitro and does not cause co

5、valent enzyme trapping inhuman cell lines. Incubation of cells with low micromolar concentrations of RG108 results in significantdemethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 causes demethylationand reactivation of tumor suppressor genes, but it does not affect th

6、e methylation of centromeric satellitesequences 1. In another study, the synthesis and in vitro analysis of a biotinylated RG108 conjugate isinvestigated to evaluate the interactions with DNA methyltransferase enzymes 2. In a recent study, it isshown RG108 can significantly reduce the DNA methyltran

7、sferases activity in SM derived iPS cells ascompared to the native SMs 3.PROTOCOLKinase Assay 1 The substrate DNA for the in vitro methylation assay is a 798 bp fragment (423/+375 relative to the initiationcodon) from the promoter region of the human p16Ink4a gene. The methylation reaction contains

8、350 to 400ng substrate DNA and 4 units of M.SssI methylase (0.5 M) in a final volume of 50 L. Inhibitors are added tofinal concentrations of 10, 100, 200, and 500 M, respectively. Reactions are done at 37C for 2 hours. Aftercompletion, the reaction is inactivated at 65C for 15 minutes and the DNA is

9、 purified using PCR Purificationkit. Three hundred nanograms of purified DNA is digested for 3 hours at 60C with 30 units of BstUI andanalyzed on 2% Tris-borate EDTA agarose gels.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Patent. US2018

10、0263995A1. Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Brueckner B, et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNAmethyltransferases. Cancer Res. 2005 Jul 15;65(14):6305-11.2. Sch

11、irrmacher E, et al. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactionswith human DNA methyltransferases. Bioconjug Chem. 2006 Mar-Apr;17(2):261-6.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. Pasha Z, et al. Efficient non-viral reprogramming of myoblasts to stemness with a single small molecule to generate cardiac progenitorcells. PLoS One. 2011;6(8):e23667.McePdfHeightCaution: Product h