Cat. No.: HY-13765

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6-Thioguanine

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

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

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

Purity: 99.54%
CAS No.: 154-42-7
Formula: C₅H₅N₅S
Molecular Weight:167.20

Storage:

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

6-Thioguanine Chemical Structure

CAS No.: 154-42-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (13)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

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

All Deubiquitinase Isoforms :

All DNA Methyltransferase Isoforms :

All Endogenous Metabolite Isoforms :

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]
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
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]
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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 154-42-7
Appearance Solid
Molecular Weight 167.20
Formula C₅H₅N₅S
Color White to yellow
SMILES

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

Thioguanine; 2-Amino-6-purinethiol
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

Publications (13)

All Cell Proliferation/Viability AssayBio/Physico-chemical AssayMicrobiological Assay

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Journal Impact Factor

Nucleic Acids Res

COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]

2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390
Redox Biol

Enteric coronavirus PDCoV evokes a non-Warburg effect by hijacking pyruvic acid as a metabolic hub. [Abstract]

2024 May:71:103112. PMID: 38461791

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).
J Immunother Cancer

Protein arginine methyltransferase 6 enhances immune checkpoint blockade efficacy via the STING pathway in MMR-proficient colorectal cancer. [Abstract]

2025 Mar 13;13(3):e010639. PMID: 40086819

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).
Cancer Lett

GSTM3 deficiency impedes DNA mismatch repair to promote gastric tumorigenesis via CAND1/NRF2-KEAP1 signaling. [Abstract]

2022 Jul 10;538:215692. PMID: 35487311
Cell Chem Biol

A base editor facilitates simultaneous purine and pyrimidine substitutions for ex vivo and in vivo mutagenesis screens. [Abstract]

2025 Sep 18;32(9):1183-1196.e5. PMID: 40912250
Transl Res

Novel MSH2 and TSC2 variants in a Chinese family with Lynch syndrome and their synergistic impact in urothelial carcinoma. [Abstract]

2024 Mar:265:26-35. PMID: 37914149
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
PLoS Negl Trop Dis

Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]

2019 Aug 20;13(8):e0007681. PMID: 31430351
Front Oncol

Hypoxanthine in the microenvironment can enable thiopurine resistance in acute lymphoblastic leukemia. [Abstract]

2024 Jul 19:14:1440650. PMID: 39099696

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).
Anim Cells Syst

Blocking SLC7A11 attenuates the proliferation of esophageal squamous cell carcinoma cells. [Abstract]

2024 May 11;28(1):237-250. PMID: 38741950
bioRxiv

OSTM1 is a ubiquitin E3 ligase that suppresses B-cell malignancy by activating the cAMP/PKA/CREB pathway. [Abstract]

2026 Jan 26:2026.01.23.701155. PMID: 41659680
bioRxiv

2025 Nov 20.
Patent

US20180263995A1.

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocol

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].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

6-Thioguanine

13 Cited Publications

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6-Thioguanine

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Publications Citing Use of MedChemExpress (MCE) 6-Thioguanine

All Deubiquitinase Isoforms

All DNA Methyltransferase Isoforms

All Endogenous Metabolite Isoforms

Biological Activity

Chemical Information

Publications (13)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

6-Thioguanine Related Classifications

HY-13765 Related Classifications