RG108  99.8049%

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包装规格:50mg 250mg in glass bottle
溶解性:溶于DMSO(100mg/mL 超声)
产品描述:基本信息 产品编号:R10125  产品名称:RG108 CAS: 48208-26-0   储存条件 粉末 -20℃ 四年     分子式: C19H14N2O4 溶于液体 -80℃ 六个月 分子量: 334.33 -20℃ 一个月 化学名:      Solubility (25°C)   体外 DMSO 66mg/mL (197.4mM) Ethanol 66mg/mL (197.4mM) Water Insoluble 体内(现配现用)     <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 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;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.9911mL 14.9553mL 29.9106mL 5mM 0.5982mL 2.9911mL 5.9821mL 10mM 0.2991mL 1.4955mL 2.9911mL 50mM 0.0598mL 0.2991mL 0.5982mL   生物活性 产品描述 一种DNMTs抑制剂,IC50:115nM,对LNCaP、22Rv1和DU145的生长抑制和凋亡诱导具有明显的剂量和时间依赖性。 靶点/IC50 DNA methyltransferase(Cell-free assay) 115nM   体外研究 RG108 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 results in significant demethylation of genomic DNA without any detectable toxicity.Intriguingly,RG108 causes demethylation and reactivation of tumor suppressor genes,but it does not affect the methylation of centromeric satellite sequences.In another study,the synthesis and in vitro analysis of a biotinylated RG108 conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes.In a recent study,it is shown RG108 can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs.   推荐实验方法(仅供参考) 激酶实验: The substrate DNA for the in vitro methylation assay is a 798 bp fragment (−423/+375 relative to the initiation codon) from the promoter region of the human p16Ink4a gene.The methylation reaction contains 350 to 400ng substrate DNA and 4 units of M.SssI methylase (0.5μM) in a final volume of 50μL.Inhibitors are added to final concentrations of 10,100,200,and 500μM,respectively. Reactions are done at 37℃ for 2 hours.After completion,the reaction is inactivated at 65℃ for 15 minutes and the DNA is purified using PCR Purification kit.Three hundred nanograms of purified DNA is digested for 3 hours at 60℃ with 30 units of BstUI and analyzed on 2% Tris-borate EDTA agarose gels.
保存条件:-20℃