6-Thioguanine (Synonyms: Thioguanine; 2-Amino-6-purinethiol)

Name: 6-Thioguanine
Brand: MedChemExpress
SKU: HY-13765
Rating: 5.0 (13 reviews)

Cat. No.: HY-13765 Purity: 99.54%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

For research use only. We do not sell to patients.

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	Get quote
5 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of 6-Thioguanine:

6-Thioguanine (Standard) In-stock
6-Thioguanine-¹³C₂,¹⁵N Get quote

13 Publications Citing Use of MCE 6-Thioguanine

Cell Proliferation/Viability Assay

Bio/Physico-chemical Assay

Microbiological Assay

: 6-Thioguanine purchased from MedChemExpress. Usage Cited in: J Immunother Cancer. 2025 Mar 13;13(3):e010639. [Abstract]; Representative images of the HPRT mutability assay in SW480 and DLD-1 cells treated with 6-Thioguanine (5 µM) were shown.

: 6-Thioguanine purchased from MedChemExpress. Usage Cited in: J Immunother Cancer. 2025 Mar 13;13(3):e010639. [Abstract]; Representative images of the HPRT mutability assay in CT26 and SW480 cells were presented. On the left, CT26 and SW480 cells were treated with 6-TG (5 µM) with or without EPZ020411 (2 µM) for 2 weeks. On the right, CT26 and SW480 cells were treated with EPZ020411 (4 µM) for 4 weeks, and the survived cells were termed CT26T or SW480T. The HPRT mutability assay was performed in CT26 and CT26T or SW480 and SW480T treated with 6-TG alone (4 µM).

: 6-Thioguanine purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 May:71:103112. [Abstract]; Cells were infected with PDCoV in media supplemented with the indicated concentrations of 6-Thioguanine (0, 1, or 5 μM).

: 6-Thioguanine purchased from MedChemExpress. Usage Cited in: Front Oncol. 2024 Jul 19:14:1440650. [Abstract]; Human plasma-like media (HPLM) attenuated leukemic cell sensitivity to thiopurine chemotherapeutics. Dose-response curves for 6-thioguanine in leukemic cells (NALM-6, REH) in regular or HPLM media were shown. Leukemic cell viability was assessed after 48 hours of drug treatment using the CellTiter-Glo Luminescent Cell Viability Assay.

: 6-Thioguanine purchased from MedChemExpress. Usage Cited in: Front Oncol. 2024 Jul 19:14:1440650. [Abstract]; Caspase-3/7 activity was assessed in leukemia cells cultured in HPLM or regular media after 48 hours of treatment with 6-Thioguanine (10 μM).

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Deubiquitinase Isoform Specific Products:

View All Isoforms

USP1 USP2 USP4 USP7 USP8 USP10 USP21 USP30 UCHL1 USP11 USP15 USP28 USP25

View All DNA Methyltransferase Isoform Specific Products:

View All Isoforms

DNA Methyltransferase DNMT1 DNMT3 MGMT

View All Endogenous Metabolite Isoform Specific Products:

View All Isoforms

Human Endogenous Metabolite Microbial Metabolite

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 25 μM (PLpros), 40 μM (Recombinant human USP2)^[3]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.82 μM Compound: 6-thioguanine	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 20605656]
ASPC1	IC₅₀	2.8 μM Compound: 6-TG	Cytotoxicity against human Aspc-1 cells by crystal violet staining Cytotoxicity against human Aspc-1 cells by crystal violet staining	[PMID: 20930123]
CCRF-CEM	EC₅₀	0.8701 μM Compound: 6-thioguanine	Cytotoxicity against human CCRF-CEM cells after 48 hrs by cell titer-blue assay Cytotoxicity against human CCRF-CEM cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
CCRF-CEM	EC₅₀	0.9416 μM Compound: 6-thioguanine	Cytotoxicity against human CCRF-CEM/C2 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human CCRF-CEM/C2 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
CCRF-CEM	IC₅₀	2.98 μM Compound: 6-thioguanine	Cytotoxicity against human CEM cells after 72 hrs by MTT assay Cytotoxicity against human CEM cells after 72 hrs by MTT assay	[PMID: 20605656]
COLO357	IC₅₀	2.09 μM Compound: 6-TG	Cytotoxicity against human Colo-357 cells by crystal violet staining Cytotoxicity against human Colo-357 cells by crystal violet staining	[PMID: 20930123]
Caco-2	CC₅₀	2.21 μM Compound: TIOGUANINE	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	1.71 μM Compound: TIOGUANINE	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
DAN-G	IC₅₀	4.32 μM Compound: 6-TG	Cytotoxicity against human DAN-G cells by crystal violet staining Cytotoxicity against human DAN-G cells by crystal violet staining	[PMID: 20930123]
HEK-293T	EC₅₀	3.6 μM Compound: 6-TG	Antiproliferative activity against HEK293T cells with high HGPRT expression incubated for 48 hrs by CellTiter-Glo2 assay Antiproliferative activity against HEK293T cells with high HGPRT expression incubated for 48 hrs by CellTiter-Glo2 assay	[PMID: 36374020]
HL-60	EC₅₀	3.897 μM Compound: 6-thioguanine	Cytotoxicity against human HL60 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human HL60 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
HL60/MX2	EC₅₀	3.649 μM Compound: 6-thioguanine	Cytotoxicity against human HL60/MX2 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human HL60/MX2 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
HT-29	IC₅₀	1240 nM Compound: Thioquanine	Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay	[PMID: 2778449]
Jurkat	GI₅₀	13 μM Compound: thioguanine	Growth inhibition of Jurkat cell Growth inhibition of Jurkat cell	[PMID: 17181155]
Jurkat	GI₅₀	147 μM Compound: thioguanine	Growth inhibition of Jurkat cell overexpressing Bcl2 Growth inhibition of Jurkat cell overexpressing Bcl2	[PMID: 17181155]
Jurkat	GI₅₀	183 μM Compound: thioguanine	Growth inhibition of Jurkat cell overexpressing BclXL Growth inhibition of Jurkat cell overexpressing BclXL	[PMID: 17181155]
K562	EC₅₀	0.74 μM Compound: 6-TG	Antiproliferative activity against human K562 cells with low HGPRT expression incubated for 48 hrs by CellTiter-Glo2 assay Antiproliferative activity against human K562 cells with low HGPRT expression incubated for 48 hrs by CellTiter-Glo2 assay	[PMID: 36374020]
K562	IC₅₀	1.54 μM Compound: 6-thioguanine	Cytotoxicity against human K562 cells after 72 hrs by MTT assay Cytotoxicity against human K562 cells after 72 hrs by MTT assay	[PMID: 20605656]
K562	IC₅₀	3.9 μM Compound: 6-thioguanine	Cytotoxicity against human paclitaxel-resistant K562 cells after 72 hrs by MTT assay Cytotoxicity against human paclitaxel-resistant K562 cells after 72 hrs by MTT assay	[PMID: 20605656]
P388	IC₅₀	300 nM Compound: Thioquanine	Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay	[PMID: 2778449]
PANC-1	IC₅₀	8.31 μM Compound: 6-TG	Cytotoxicity against human PANC1 cells by crystal violet staining Cytotoxicity against human PANC1 cells by crystal violet staining	[PMID: 20930123]
PaTu 8988t	IC₅₀	3.43 μM Compound: 6-TG	Cytotoxicity against human Patu-T cells by crystal violet staining Cytotoxicity against human Patu-T cells by crystal violet staining	[PMID: 20930123]
THP-1	EC₅₀	0.27 μM Compound: 6-TG	Antiproliferative activity against human THP-1 cells with low HGPRT expression incubated for 48 hrs by CellTiter-Glo2 assay Antiproliferative activity against human THP-1 cells with low HGPRT expression incubated for 48 hrs by CellTiter-Glo2 assay	[PMID: 36374020]
Vero C1008	CC₅₀	35.5 μM Compound: 26	Cytotoxicity against African green monkey Vero E6 cells assessed as cell viability Cytotoxicity against African green monkey Vero E6 cells assessed as cell viability	[PMID: 35620927]

In Vitro

6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC₅₀s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively^[1]. 6-Thioguanine (Thioguanine) affects the methylation of cytosine residues by purified DNA methyltransferases including human DNMT1 and bacterial HpaII methylase. 6-Thioguanine (Thioguanine) (1 or 3 μM) decreases global cytosine methylation in Jurkat T cells and cytosine methylation in human cells at 3 μM^[2]. 6-Thioguanine (Thioguanine) (18.75, 37.50, or 75.00 μM) adversely affects cell viability, but with no effect on LDH or ALT activity^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

167.20

Formula

C₅H₅N₅S

CAS No.

154-42-7

Appearance

Solid

Color

White to yellow

SMILES

SC1=NC(N)=NC2=C1N=CN2

Structure Classification

Others

Initial Source

Endogenous metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

1 M NaOH : ≥ 100 mg/mL (598.09 mM)

DMSO : 10 mg/mL (59.81 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	5.9809 mL	29.9043 mL	59.8086 mL
5 mM	1.1962 mL	5.9809 mL	11.9617 mL
10 mM	0.5981 mL	2.9904 mL	5.9809 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (9.99 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.54%

Select Batch:

Data Sheet (278 KB) SDS (480 KB)

COA (244 KB) RP-HPLC (207 KB)

Handling Instructions (2659 KB)

References

[1]. Chuang SJ, et al. 6-Thioguanine is a noncompetitive and slow binding inhibitor of human deubiquitinating protease USP2. Sci Rep. 2018 Feb 15;8(1):3102. [Content Brief]

[2]. Wang H, et al. 6-Thioguanine perturbs cytosine methylation at the CpG dinucleotide site by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo. Biochemistry. 2009 Mar 17;48(10):2290-9. [Content Brief]

[3]. LaDuke KE, et al. Effects of azathioprine, 6-mercaptopurine, and 6-thioguanine on canine primary hepatocytes. Am J Vet Res. 2015 Jul;76(7):649-55. [Content Brief]

Cell Assay
^[3]

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^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Chuang SJ, et al. 6-Thioguanine is a noncompetitive and slow binding inhibitor of human deubiquitinating protease USP2. Sci Rep. 2018 Feb 15;8(1):3102. [Content Brief]

[2]. Wang H, et al. 6-Thioguanine perturbs cytosine methylation at the CpG dinucleotide site by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo. Biochemistry. 2009 Mar 17;48(10):2290-9. [Content Brief]

[3]. LaDuke KE, et al. Effects of azathioprine, 6-mercaptopurine, and 6-thioguanine on canine primary hepatocytes. Am J Vet Res. 2015 Jul;76(7):649-55. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / 1 M NaOH	1 mM	5.9809 mL	29.9043 mL	59.8086 mL	149.5215 mL
	5 mM	1.1962 mL	5.9809 mL	11.9617 mL	29.9043 mL
	10 mM	0.5981 mL	2.9904 mL	5.9809 mL	14.9522 mL
	15 mM	0.3987 mL	1.9936 mL	3.9872 mL	9.9681 mL
	20 mM	0.2990 mL	1.4952 mL	2.9904 mL	7.4761 mL
	25 mM	0.2392 mL	1.1962 mL	2.3923 mL	5.9809 mL
	30 mM	0.1994 mL	0.9968 mL	1.9936 mL	4.9841 mL
	40 mM	0.1495 mL	0.7476 mL	1.4952 mL	3.7380 mL
	50 mM	0.1196 mL	0.5981 mL	1.1962 mL	2.9904 mL
1 M NaOH	60 mM	0.0997 mL	0.4984 mL	0.9968 mL	2.4920 mL
	80 mM	0.0748 mL	0.3738 mL	0.7476 mL	1.8690 mL
	100 mM	0.0598 mL	0.2990 mL	0.5981 mL	1.4952 mL

6-Thioguanine Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

6-Thioguanine154-42-7Thioguanine 2-Amino-6-purinethiolSARS-CoVDeubiquitinaseDNA MethyltransferaseAutophagyApoptosisEndogenous MetaboliteSARS coronavirusDUBsDNMTsDNA MTasesInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Product Name			Requested Quantity *
Applicant Name *			Salutation
Email Address *			Phone Number *
Department			Organization Name *
City			State
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

6-Thioguanine (Synonyms: Thioguanine; 2-Amino-6-purinethiol)

Customer Review

Other Forms of 6-Thioguanine:

6-Thioguanine Related Antibodies

13 Publications Citing Use of MCE 6-Thioguanine

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Deubiquitinase Isoform Specific Products:

View All DNA Methyltransferase Isoform Specific Products:

View All Endogenous Metabolite Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

6-Thioguanine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

6-Thioguanine Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report