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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE6-ThioguanineCat. No.: HY-13765CAS No.: 154-42-7Synonyms: Thioguanine;2-Amino-6-purinethiol分式: CHNS分量: 167.19作靶點(diǎn): SARS-CoV; Deubiquitinase; Autophagy作通路: Anti-infection; Cell Cycle/DNA Damage; Autophagy儲(chǔ)存式: Powder -20C 3 years4C
2、 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 10 mg/mL (59.81 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 5.9812 mL 29.9061 mL 59.8122 mL5 mM 1.1962 mL 5.9812 mL 11.9624 mL10 mM 0.5981 mL 2.9906 mL 5.9812 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲(chǔ)備液,并請(qǐng)注意儲(chǔ)備液的保存
3、式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液,再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性,體內(nèi)實(shí)驗(yàn)的作液,建議您現(xiàn)現(xiàn)配,當(dāng)天使;澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)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(qǐng)依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1.67 mg/mL (9.99 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.Med
4、ChemE物活性 6-Thioguanine (Thioguanine)種抗病和免疫抑制劑,為 SARS 和 MERS 冠狀病毒樣蛋酶 (PLpros) 的抑制劑,同時(shí)可有效抑制 USP2 的活性,IC50 值分別為 25 M 和 40 M。IC50 & Target IC50: 25 M (PLpros), 40 M (Recombinant human USP2) 3體外研究 6-Thioguanine (Thioguanine) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARSand
5、 MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of25 M and 40 M for Plpros and recombinant human USP2, respectively 1. 6-Thioguanine (Thioguanine)affects the methylation of cytosine residues by purified DNA methyltransferases including human DNMT
6、1 andbacterial HpaII methylase. 6-Thioguanine (Thioguanine) (1 or 3 M) decreases global cytosine methylation inJurkat T cells and cytosine methylation in human cells at 3 M 2. 6-Thioguanine (Thioguanine) (18.75, 37.50,or 75.00 M) adversely affects cell viability, but with no effect on LDH or ALT act
7、ivity 3.PROTOCOLCell Assay 3 Treatments consists of 3 thiopurines (azathioprine, 6-mercaptopurine, and 6-Thioguanine (Thioguanine) ateach of 6 concentrations (0.468, 0.937, 1.875, 3.750, 7.500, and 15.000 M). Each thiopurinee is dissolvedin DMSO solution to achieve a concentration of 10 mg/mL. Steri
8、le filtered maintenance medium is used tofurther dilute each thiopurine solution to each of the 6 treatment concentrations. Twenty-four hours after thehepatocytes are plated on 96-well culture 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研
9、獻(xiàn) Patent. US20180263995A1.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Chuang SJ, et al. 6-Thioguanine is a noncompetitive and slow binding inhibitor of human deubiquitinating protease USP2. Sci Rep. 2018Feb 15;8(1):3102.2. Wang H, et al. 6-Thioguanine perturbs cytosine meth
10、ylation at the CpG dinucleotide site by DNA methyltransferases in vitro and acts asa DNA demethylating agent in vivo. Biochemistry. 2009 Mar 17;48(10):2290-9.3. LaDuke KE, et al. Effects of azathioprine, 6-mercaptopurine, and 6-thioguanine on canine primary hepatocytes. Am J Vet Res. 2015Jul;76(7):649-55.McePdfHeightCaution: Product has not been fully vali
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