| CAS |
154-42-7 |
| Chinese Name |
6-硫鸟嘌呤 |
| English Name |
6-Thioguanine |
| Synonyms |
6-硫代鸟嘌呤;4-Penylbutan-2-one;6-硫鸟嘌呤;Apacz; |
| Molecular Formula |
C5H5N5S |
| Molecular Weight |
167.19 |
| Solubility |
Soluble in DMSO |
| Purity |
≥98% |
| Appearance |
White to yellow Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 205-827-2 |
| MDL |
MFCD00233553 |
| SMILES |
SC1=NC(N)=NC2=C1N=CN2 |
| InChIKey |
WYWHKKSPHMUBEB-UHFFFAOYSA-N |
| InChI |
InChI=1S/C5H5N5S/c6-5-9-3-2(4(11)10-5)7-1-8-3/h1H,(H4,6,7,8,9,10,11) |
| PubChem CID |
2723601 |
| Target Point |
Influenza Virus(SARS-CoV) |
| Passage |
Anti-infection |
| Background |
6-Thioguanine is an immunosuppressant and an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros), and can effectively inhibit the activity of USP2. Can be used for anti-leukemia related research. |
| Biological Activity |
6-Thioguanine 是一种抗白血病和免疫抑制剂, 为 SARS 和 MERS 冠状病毒木瓜样蛋白酶 (PLpros) 的抑制剂, 同时可有效抑制 USP2 的活性, IC50 值分别为 25 μM 和 40 μM[3]。 |
| IC50 |
IC50: 25μM (PLpros) ， 40μM (Recombinant human USP2) [3] |
| In Vitro |
6-Thioguanine是一种抗白血病和免疫抑制剂，可作为SARS和MERS冠状病毒木瓜蛋白酶样蛋白酶(PLpros)的抑制剂，并有效抑制USP2活性，对于Plpros和重组人USP2，IC50为25μM和40μM，分别[1]。 6-硫鸟嘌呤通过纯化的DNA甲基转移酶(包括人DNMT1和细菌HpaII甲基化酶)影响胞嘧啶残基的甲基化。 6-Thioguanine(1或3μM)降低Jurkat T细胞中的全局胞嘧啶甲基化和3μM人细胞中的胞嘧啶甲基化[2]。 6-硫鸟嘌呤(18.75，37.50或75.00μM)对细胞活力产生不利影响，但对LDH或ALT活性没有影响[3]。 |
| Cell Experiment |
治疗由6种浓度(0.468，0.937，1.875，3.750，7.500和15.000μM)中的3种硫代嘌呤(硫唑嘌呤，6-巯基嘌呤和6-硫鸟嘌呤)组成。将每种硫嘌呤溶解在DMSO溶液中以达到10mg / mL的浓度。使用无菌过滤的维持培养基将每种硫嘌呤溶液进一步稀释至6种处理浓度中的每一种。将肝细胞接种于96孔培养物后24小时[3]。 |
| Data Literature Source |
[1]. Chuang SJ， et al. 6-Thioguanine is a noncompetitive and slow binding inhibitor of human deubiquitinating protease USP2. Sci Rep. 2018 Feb 15; 8 (1) :3102.
[2]. Wang H， et al. 6-Thioguanine perturbs cytosine methylation at the CpG dinucleotide site by DNA methyltransferases in vitro and acts as a 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. 2015 Jul; 76 (7) :649-55 |
| Unit |
Bottle |
| Specification |
50mg 10mM*1mL in DMSO 100mg |
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