product name Thioguanine
Description: Thioguanine, also known as AAN, USAN, and 6-TG, is a purine antimetabolite that inhibits DNMT1 activity through ubiquitin-targeted degradation, it has been used in the treatment of acute lymphoblastic leukemia, autoimmune disorders (e.g., Crohns disease, rheumatoid arthritis) and organ transplant recipients. However, thioguanine has been used less frequently in recent years because of safety concerns. However, it is becoming more widely used for treating ulcerative colitis and some autoimmune diseases.
References: FASEB J. 2000 Nov;14(14):2339-44; Cancer Res. 2010 Aug 1;70(15):6268-76.
167.19
Formula
C5H5N5S
CAS No.
154-42-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19410944
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | 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 |
| Animal model | |
| Formulation & Dosage | |
| References | FASEB J. 2000 Nov;14(14):2339-44; Cancer Res. 2010 Aug 1;70(15):6268-76. |
