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Thioguanine DNA Methyltransferase inhibitor

Name: Thioguanine
Brand: Selleck Chemicals
SKU: S1774
Availability: InStock
Rating: 5 (25 reviews)

Cat.No.S1774

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.

Chemical Structure

Molecular Weight: 167.19

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Quality Control

Batch: Purity: 99.93%

99.93

Related Targets	HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK
Other DNA Methyltransferase Products	RG108 SGI-1027 Zebularine (NSC 309132) Gamma-Oryzanol CM272 GSK3685032 β-thujaplicin GSK-3484862 SF3B1 Antibody [G23D1] DNMT3A Antibody [E19E6]

Solubility

In vitro
Batch:

DMSO : 17 mg/mL (101.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 40%PEG300 2 2%Tween80 3 56%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (5.98mM)	Taking the 1 mL working solution as an example, add 20 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 560 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	167.19	Formula	C₅H₅N₅S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	154-42-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 752, 6-Thioguanine, 2-Amino-6-purinethiol			Smiles	C1=NC2=C(N1)C(=S)N=C(N2)N

Mechanism of Action

Targets/IC₅₀/Ki	DNMT1
In vitro	Thioguanine incorporation alters the DNA cleavage induced by topoisomerase II in the presence and absence of etoposide. This compound alters the structure and lowers the thermal stability of duplex DNA, but duplex DNA can be formed in the presence of 6SG. Its induced apopotosis is similarly observed in both mismatch repair-proficient and -deficient HCT116 and HeLa cells. This chemical integrates into DNA and unlike the canonical DNA bases, it is a strong UVA chromophore with an absorbance maximum at 342 nm. It is a photosensitizer and a source of reactive oxygen species. In canine lymphoma cells, this compound 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. This compound efficiently kills such BRCA1-defective PARP inhibitor-resistant tumors. It could kill cells and tumors that have gained resistance to PARP inhibitors or cisplatin through genetic reversion of the BRCA2 gene.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11053256/ [2] https://pubmed.ncbi.nlm.nih.gov/10390526/ [3] https://pubmed.ncbi.nlm.nih.gov/15788687/ [4] https://pubmed.ncbi.nlm.nih.gov/20631063/ [5] https://pubmed.ncbi.nlm.nih.gov/20631063/ [6] https://pubmed.ncbi.nlm.nih.gov/25480665/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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