1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGJ103 sodium saltCat. No.: HY-101203ACAS No.: 1459687-96-7分式: CHNNaOS分量: 364.35作靶點: Others作通路: Others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 : 34 mg/mL (93.32 mM)* means soluble, but

2、saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.7446 mL 13.7231 mL 27.4461 mL5 mM 0.5489 mL 2.7446 mL 5.4892 mL10 mM 0.2745 mL 1.3723 mL 2.7446 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。BIOLOGICAL ACTIVITY物活性 GJ103 sodium salt是通讀化合物GJ072的活性類似物。體外研究Chemical-induced read th

3、rough of premature stop codons might be exploited as a potential treatmentstrategy for genetic disorders caused by nonsense mutations. GJ072 is a novel read-through compound(RTC). GJ072 shows activity comparable to stop codons (TGA, TAG, and TAA) PTC124 and RTC13. GJ072induces ATM kinase on both TGA

4、 and TAG stop codons and restored ATMpSer1981 autophosphorylation1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEand SMC1pSer966 transphosphorylation as measured by FACS. GJ072 is active in A-T cells with ahomozygous TAA mutation. GJ072 is able to induce detectable full-length ATM protein in treate

5、d A-T cells.Early structure-activity relationship studies generates eight active analogs of GJ072. Some GJ072 analogs(e.g., GJ103, GJ106, GJ109, and GJ111) consistently demonstrates their activities in all three PTCs by bothFCATMpSer1981 and IRIF assays. GJ071 and GJ072 and some of their analogs (su

6、ch as GJ103) havesimilar read-through activity as RTC13 or RTC14, but are more tolerable than RTC13 and RTC14 to A-Tcells. GJ103 does not show obvious cytotoxicity in A-T cells at concentration as high as 300 M 1.體內研究 GJ103 sodium salt is water soluble, making it much easier to work with in in vivo

7、experiments 1.PROTOCOLCell Assay 1 Cytotoxicity is measured by cell proliferation assay. Cells are seeded into a flat-bottom 96-well plate,including control wells containing complete growth medium alone as blank absorbance readings. After RTCtreatment (GJ103), activated-XTT Solution is added into ea

8、ch well, and the cells are returned to the cellculture incubator for 12-14 hours. The absorbance is measured at 480 nM with relevant 630 nM to assessnonspecific readings 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Du L, et al. A new series of small molecular weight compounds induce read through of all three types of nonsense mutations in the ATMgene. Mol Ther. 2013 Sep;21(9):1653-60.McePdfHeightCaution: Product has not been fully validated for medical appl