RG108-N-Phthalyl-L-tryptophan-DataSheet-生命科學試劑-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作靶點: DNA Methyltransferase作通路: Epigenetics儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 100 mg

2、/mL (299.11 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解案，配制前請先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的作液，建議您現

3、現配，當天使；澄清的儲備液可以根據儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.48 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.48 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master o

4、f Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (7.48 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 RG108種核苷的 DNA 甲基轉移酶 (DNA methyltransferase) 抑制劑，IC50 值為 115 nM。IC50 & Target CpG methylase M.SssI115 nM (IC50)體外研究 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.戶使本產品發(fā)表的科研獻 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 您邊的抑制劑師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