Thioguanine (NSC 752)

Catalog No.S1774 Synonyms: 6-Thioguanine, 2-Amino-6-purinethiol

For research use only.

Thioguanine (NSC 752, 6-Thioguanine, 2-Amino-6-purinethiol), 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 (NSC 752) Chemical Structure

CAS No. 154-42-7

Selleck's Thioguanine (NSC 752) has been cited by 16 publications

Purity & Quality Control

Choose Selective DNA Methyltransferase Inhibitors

Biological Activity

Description Thioguanine (NSC 752, 6-Thioguanine, 2-Amino-6-purinethiol), 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.
Targets
DNMT1 [6]
()
In vitro

Thioguanine incorporation alters the DNA cleavage induced by topoisomerase II in the presence and absence of etoposide. [1] 6-Thioguanine alters the structure and lowers the thermal stability of duplex DNA, but duplex DNA can be formed in the presence of 6SG. [2] 6-Thioguanine induced apopotosis is similarly observed in both mismatch repair-proficient and -deficient HCT116 and HeLa cells. [3] 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. [4] In canine lymphoma cells, Thioguanine significantly decreases DNMT1 protein and global DNA methylation. [6]

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. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 9 mg/mL
(53.83 mM)
Water Insoluble
Ethanol Insoluble

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.

1mg/mL

Chemical Information

Molecular Weight 167.19
Formula

C5H5N5S

CAS No. 154-42-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=NC2=C(N1)C(=S)N=C(N2)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03022747 Unknown status Drug: Allopurinol|Drug: Standard treatment Lymphoblastic Leukemia Acute Childhood Vastra Gotaland Region January 2017 Phase 2
NCT04304950 Recruiting Drug: Evening Group|Drug: Morning Group Inflammatory Bowel Diseases Rush University Medical Center April 25 2016 Phase 4
NCT00548431 Completed Drug: 6-mercaptopurine Leukemia Lymphocytic Acute Rigshospitalet Denmark December 2007 Phase 2
NCT00098111 Terminated Drug: azathioprine Crohn''s Disease Massachusetts General Hospital April 2005 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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