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||9 mg/mL (53.83 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01190930||Active not recruiting||Acute Lymphoblastic Leukemia|Adult B Lymphoblastic Lymphoma|Ann Arbor Stage I B Lymphoblastic Lymphoma|Ann Arbor Stage II B Lymphoblastic Lymphoma|Childhood B Acute Lymphoblastic Leukemia|Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1|Childhood B Lymphoblastic Lymphoma|Down Syndrome|Hypodiploid B Acute Lymphoblastic Leukemia|Intrachromosomal Amplification of Chromosome 21|Philadelphia Chromosome Positive|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia||Children''s Oncology Group|National Cancer Institute (NCI)||August 9 2010||Phase 3|
|NCT02101853||Recruiting||B Acute Lymphoblastic Leukemia||National Cancer Institute (NCI)||December 8 2014||Phase 3|
|NCT03571321||Not yet recruiting||Acute Lymphoblastic Leukemia|ALL Childhood|ALL||University of Chicago|Incyte Corporation||September 5 2019||Phase 1|
|NCT02112916||Suspended||Adult T Acute Lymphoblastic Leukemia|Ann Arbor Stage II Adult Lymphoblastic Lymphoma|Ann Arbor Stage II Childhood Lymphoblastic Lymphoma|Ann Arbor Stage III Adult Lymphoblastic Lymphoma|Ann Arbor Stage III Childhood Lymphoblastic Lymphoma|Ann Arbor Stage IV Adult Lymphoblastic Lymphoma|Ann Arbor Stage IV Childhood Lymphoblastic Lymphoma|Childhood T Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia||National Cancer Institute (NCI)||September 30 2014||Phase 3|
|NCT00549848||Active not recruiting||Acute Lymphoblastic Leukemia||St. Jude Children''s Research Hospital|National Cancer Institute (NCI)|Enzon Pharmaceuticals Inc.|National Institute of General Medical Sciences (NIGMS)||October 29 2007||Phase 3|
|NCT03007147||Recruiting||B Acute Lymphoblastic Leukemia|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||Children''s Oncology Group|National Cancer Institute (NCI)||July 28 2017||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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