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  2. Anti-infection Cell Cycle/DNA Damage Epigenetics Autophagy Apoptosis Metabolic Enzyme/Protease
  3. SARS-CoV Deubiquitinase DNA Methyltransferase Autophagy Apoptosis Endogenous Metabolite
  4. 6-Thioguanine

6-Thioguanine  (Synonyms: 硫鳥嘌呤; Thioguanine; 2-Amino-6-purinethiol)

目錄號(hào): HY-13765 純度: 99.90%
COA 產(chǎn)品使用指南 技術(shù)支持

6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) 是一種抗白血病和免疫抑制劑，為 SARS 和 MERS 病毒木瓜樣蛋白酶 (PLpros) 的抑制劑，同時(shí)可有效抑制 USP2 的活性，IC50 值分別為 25 μM 和 40 μM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

6-Thioguanine Chemical Structure

6-Thioguanine Chemical Structure

CAS No. : 154-42-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥537
In-stock
100 mg ￥488
In-stock
500 mg ￥900
In-stock
1 g   詢價(jià)  
5 g   詢價(jià)  

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Customer Review

Other Forms of 6-Thioguanine:

查看 Deubiquitinase 亞型特異性產(chǎn)品:

查看 DNA Methyltransferase 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

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.

IC50 & Target

IC50: 25 μM (PLpros), 40 μM (Recombinant human USP2)[3]
細(xì)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]
體外研究
(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 號(hào)
性狀

固體

顏色

White to yellow

中文名稱

硫鳥嘌呤
結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 10 mg/mL (59.81 mM; 超聲加熱助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.67 mg/mL (9.99 mM); 澄清溶液

    此方案可獲得 ≥ 1.67 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 16.7 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.90%

參考文獻(xiàn)
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.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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
Help & FAQs
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    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.

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產(chǎn)品名稱：
6-Thioguanine
目錄號(hào)：
HY-13765
需求量：