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Submit Review6-Thioguanine is an anticancer and immunosuppressive agent often used to treat immune disorders and leukemia. Displays cytotoxic and antineoplastic properties; disrupts cytosine methylation by DNA methyltransferases after incorporation into DNA. Selectively kills BRCA2-defective tumors in a xenograft model. Also facilitates proteasome-mediated degradation of DNA (cytosine-5)-methyltransferase 1 (DNMT1). Also inhibits SARS-CoV papain-like protease (PLpro; IC50 = 5 μM for PLpro deubiquitination activity).
分子量 | 167.19 |
公式 | C5H5N5S |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 154-42-7 |
PubChem ID | 2723601 |
InChI Key | WYWHKKSPHMUBEB-UHFFFAOYSA-N |
Smiles | NC1=NC(S)=C2C(NC=N2)=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 16.72 | 100 |
以下数据基于产品分子量 167.19。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 5.98 mL | 29.91 mL | 59.81 mL |
5 mM | 1.2 mL | 5.98 mL | 11.96 mL |
10 mM | 0.6 mL | 2.99 mL | 5.98 mL |
50 mM | 0.12 mL | 0.6 mL | 1.2 mL |
参考文献是支持产品生物活性的出版物。
Wang and Wang (2009) 6-Thioguanine perturbs cytosine methylation at CgP dinucleotide site by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo. Biochemistry 48 2290 PMID: 19236003
Issaeva et al (2010) 6-Thioguanine selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance. Cancer Res. 70 6268 PMID: 20631063
Yuan et al (2011) 6-thioguanine reactivates epigenetically silenced genes in acute lymphoblastic leukemia cells by facilitating proteasome-mediated degradation of DNMT1. Cancer Res. 71 1904 PMID: 21239472
If you know of a relevant reference for 6-Thioguanine, please let us know.
关键词: 6-Thioguanine, 6-Thioguanine supplier, 6-TG, anticancer, chemotherapeutics, immunosupprressive, agents, cytotoxic, antineoplastic, cancer, BRCA2, tumors, epigenetics, antimetabolites, DNA, Methyltransferases, Immunosuppressants, Papain-like, Proteases, 4061, Tocris Bioscience
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