Molecular Weight(MW): 167.19
Thioguanine, a purine antimetabolite, inhibits DNMT1 activity through ubiquitin-targeted degradation, used in the treatment of acute lymphoblastic leukemia, autoimmune disorders (e.g., Crohn's disease, rheumatoid arthritis) and organ transplant recipients.
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Choose Selective DNA Methyltransferase Inhibitors
|Description||Thioguanine, a purine antimetabolite, inhibits DNMT1 activity through ubiquitin-targeted degradation, used in the treatment of acute lymphoblastic leukemia, autoimmune disorders (e.g., Crohn's disease, rheumatoid arthritis) and organ transplant recipients.|
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. 
|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. |
-  Krynetskaia NF, et al. FASEB J,?000, 14(14), 2339-2344.
-  Marathias VM, et al. Nucleic Acids Res,?999, 27(14), 2860-2867.
-  Yamane K, et al. Clin Cancer Res,?005, 11(6), 2355-2363.
|In vitro||DMSO||17 mg/mL warmed (101.68 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03007147||Not yet recruiting||B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1|BCR-ABL1 Fusion Protein Expression|Minimal Residual Disease|Philadelphia Chromosome Positive|T Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia||Childrens Oncology Group|National Cancer Institute (NCI)||July 2017||Phase 3|
|NCT02828358||Not yet recruiting||Acute Leukemia of Ambiguous Lineage|Childhood B Acute Lymphoblastic Leukemia|Mixed Phenotype Acute Leukemia||National Cancer Institute (NCI)||December 2016||--|
|NCT02912676||Recruiting||Acute Lymphoblastic Leukemia||Kjeld Schmiegelow|Danish Child Cancer Foundation|Nordic Society for Pediatric Hematology and Oncology|Rigshospitalet, Denmark||October 2016||Phase 1|Phase 2|
|NCT02723994||Recruiting||B-cell Acute Lymphoblastic Leukemia||Incyte Corporation|Childrens Oncology Group||August 2016||Phase 2|
|NCT02419469||Recruiting||Leukemia|Precursor-B Acute Lymphoblastic Leukemia|Lymphoblastic Lymphoma|Lymphoma||M.D. Anderson Cancer Center|Jazz Pharmaceuticals||November 2015||Phase 2|
|NCT02521493||Recruiting||Childhood Acute Myeloid Leukemia|Childhood Myelodysplastic Syndrome|Cytopenia|Down Syndrome|Myeloid Leukemia Associated With Down Syndrome|Myeloproliferative Neoplasm||Childrens Oncology Group|National Cancer Institute (NCI)||November 2015||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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