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    Thioguanine (NSC-752; Tabloid)
    Thioguanine (NSC-752; Tabloid)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0406
    CAS #: 154-42-7Purity ≥98%

    Description: Thioguanine (6-Thioguanine; NSC752; Tabloid; 2-Amino-6-purinethiol; 6-TG), an FDA approved medication used for treating AML-acute myeloid leukemia, is an antimetabolite anticancer drug, specifically, an anti-leukemia and immunosuppressant agent. It acts by inhibiting DNMT1 activity through ubiquitin-targeted degradation.

    ReferencesFASEB J. 2000 Nov;14(14):2339-44; Cancer Res. 2010 Aug 1;70(15):6268-76.

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    Thioguanine

    Name: Thioguanine
    CAS#: 154-42-7
    Chemical Formula: C5H5N5S
    Exact Mass: 167.02657
    Molecular Weight: 167.19
    Elemental Analysis: C, 35.92; H, 3.01; N, 41.89; S, 19.18
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: 2-Amino-6-purinethiol; thioguanine; ThioguanineTabloid; Tioguanine. Lanvis; Tioguanin; 6TG; TG. BW 5071; WR1141; X 27.
    Chemical Name: 2-amino-1H-purine-6(7H)-thione
    InChi Key: WYWHKKSPHMUBEB-UHFFFAOYSA-N
    InChi Code: InChI=1S/C5H5N5S/c6-5-9-3-2(4(11)10-5)7-1-8-3/h1H,(H4,6,7,8,9,10,11)
    SMILES Code: S=C1NC(N)=NC2=C1NC=N2


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    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.


    Cell Assay: Treatments consists of 3 thiopurines (azathioprine, 6-mercaptopurine, and 6-Thioguanine (Thioguanine)) at each of 6 concentrations (0.468, 0.937, 1.875, 3.750, 7.500, and 15.000 μM). Each thiopurinee is dissolved in DMSO solution to achieve a concentration of 10 mg/mL. Sterile filtered maintenance medium is used to further dilute each thiopurine solution to each of the 6 treatment concentrations. Twenty-four hours after the hepatocytes are plated on 96-well culture

    In VivoThioguanine 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 modelNA
    Formulation & DosageNA
    References

    FASEB J. 2000 Nov;14(14):2339-44; Cancer Res. 2010 Aug 1;70(15):6268-76.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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