6-Thioguanine (Synonyms: 硫鸟嘌呤; Thioguanine; 2-Amino-6-purinethiol)

目录号: HY-13765 纯度: 98.01%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) 是一种抗白血病和免疫抑制剂，为 SARS 和 MERS 病毒木瓜样蛋白酶 (PLpros) 的抑制剂，同时可有效抑制 USP2 的活性，IC₅₀ 值分别为 25 μM 和 40 μM。

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6-Thioguanine Chemical Structure

CAS No. : 154-42-7

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥537	In-stock
100 mg	￥488	In-stock
500 mg	￥900	In-stock
1 g		询价
5 g		询价

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Customer Review

Other Forms of 6-Thioguanine:

6-Thioguanine (Standard) 询价

MCE 顾客使用本产品发表的 9 篇科研文献

6-Thioguanine 相关产品

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USP1 USP2 USP7 USP8 USP30 UCHL1

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DNA Methyltransferase DNMT1 DNMT3 MGMT

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

IC₅₀ & Target

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

细胞效力
(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	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
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
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]
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]

体外研究
(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].

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

Clinical Trial

分子量

167.19

Formula

C₅H₅N₅S

CAS 号

154-42-7

性状

固体

颜色

White to yellow

中文名称

硫鸟嘌呤

结构分类

Others

初始来源

内源性代谢物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 10 mg/mL (59.81 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	5.9812 mL	29.9061 mL	59.8122 mL
5 mM	1.1962 mL	5.9812 mL	11.9624 mL
10 mM	0.5981 mL	2.9906 mL	5.9812 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (9.99 mM); 澄清溶液

此方案可获得 ≥ 1.67 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 98.01%

选择批次：

Data Sheet (626 KB) SDS (420 KB)

COA (265 KB) RP-HPLC (200 KB) MS (80 KB)

产品使用指南 (1538 KB)

参考文献

[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.
参考文献	[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.

参考文献

[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]

6-Thioguanine 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	5.9812 mL	29.9061 mL	59.8122 mL	149.5305 mL
	5 mM	1.1962 mL	5.9812 mL	11.9624 mL	29.9061 mL
	10 mM	0.5981 mL	2.9906 mL	5.9812 mL	14.9530 mL
	15 mM	0.3987 mL	1.9937 mL	3.9875 mL	9.9687 mL
	20 mM	0.2991 mL	1.4953 mL	2.9906 mL	7.4765 mL
	25 mM	0.2392 mL	1.1962 mL	2.3925 mL	5.9812 mL
	30 mM	0.1994 mL	0.9969 mL	1.9937 mL	4.9843 mL
	40 mM	0.1495 mL	0.7477 mL	1.4953 mL	3.7383 mL
	50 mM	0.1196 mL	0.5981 mL	1.1962 mL	2.9906 mL

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Keywords:

6-Thioguanine154-42-7Thioguanine 2-Amino-6-purinethiol硫鸟嘌呤SARS-CoVDeubiquitinaseDNA MethyltransferaseAutophagyApoptosisEndogenous MetaboliteSARS coronavirusDUBsDNMTsDNA MTasesInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

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上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

6-Thioguanine (Synonyms: 硫鸟嘌呤; Thioguanine; 2-Amino-6-purinethiol)

Customer Review

Other Forms of 6-Thioguanine:

MCE 顾客使用本产品发表的 9 篇科研文献