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抑制剂描述:

产品名称:6-Thioguanine

产品别名:见爱必信官网

英文别名:6-Thioguanine

靶点:DNA Methyltransferase

CAS:154-42-7

纯度:≥98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

6-Thioguanine is a chemotherapy drug that demonstrates immunosuppressive, anti-neoplastic, and anti-cancer activities. This chemical is often used to treat leukemia and inflammatory diseases. Chemical produces dose-dependent inhibition of stimulated expression of TRAIL protein.

溶解性:DMSO : 14 mg/mL (83.7 mM)

体外研究:

Thioguanine incorporation alters the DNA cleavage induced by topoisomerase II in the presence and absence of etoposide. 6-Thioguanine alters the structure and lowers the thermal stability of duplex DNA, but duplex DNA can be formed in the presence of 6SG. 6-Thioguanine induced apopotosis is similarly observed in both mismatch repair-proficient and -deficient HCT116 and HeLa cells. Thioguanine integrates into DNA and unlike the canonical DNA bases, it is a strong UVA chromophore with an absorbance maximum at 342 nm. 6-Thioguanine is a photosensitizer and a source of reactive oxygen species. In canine lymphoma cells, Thioguanine significantly decreases DNMT1 protein and global DNA methylation.

体内研究:Thioguanine is as efficient as a PARP inhibitor in selectively killing BRCA2-defective tumors in a xenograft model. 6-Thioguanine efficiently kills such BRCA1-defective PARP inhibitor-resistant tumors. 6-Thioguanine could kill cells and tumors that have gained resistance to PARP inhibitors or cisplatin through genetic reversion of the BRCA2 gene.

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