Home Epigenetics DNA Methyltransferase inhibitor Thioguanine For research use only.

Thioguanine

Synonyms: NSC 752, 6-Thioguanine, 2-Amino-6-purinethiol

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 Chemical Structure

Thioguanine Chemical Structure

CAS No. 154-42-7

Purity & Quality Control

Thioguanine Related Products

Signaling Pathway

DNA Methyltransferase Signaling Pathways

DNA Methyltransferase Signaling Pathway

Biological Activity

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.
Targets
DNMT1 [6]
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03022747 Unknown status
Lymphoblastic Leukemia Acute Childhood
Vastra Gotaland Region
 January 2017 Phase 2
NCT04304950 Completed
Inflammatory Bowel Diseases
Rush University Medical Center
 April 25 2016 Phase 4
NCT00548431 Completed
Leukemia Lymphocytic Acute
Rigshospitalet Denmark
 December 2007 Phase 2
NCT00098111 Terminated
Crohn''s Disease
Massachusetts General Hospital
 April 2005 Phase 3

Chemical Information & Solubility

Molecular Weight 167.19 Formula

C5H5N5S
CAS No. 154-42-7 SDF Download Thioguanine SDF
Smiles C1=NC2=C(N1)C(=S)N=C(N2)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 17 mg/mL ( (101.68 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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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.

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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