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/ 6-Thioguanine/6-硫鸟嘌呤

6-Thioguanine/6-硫鸟嘌呤 {[allProObj[0].p_purity_real_show]}

货号：A393548 同义名： 硫鸟嘌呤 / Thioguanine; 2-Amino-6-purinethiol

6-Thioguanine 是一种抗白血病化合物，抑制 SARS 和 MERS 病毒木瓜样蛋白酶 (PLpro)，IC50 为 25 μM，并作为 DNA 去甲基化剂。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
6-Thioguanine/6-硫鸟嘌呤 化学结构 CAS号：154-42-7
6-Thioguanine/6-硫鸟嘌呤 化学结构
CAS号：154-42-7
6-Thioguanine/6-硫鸟嘌呤 3D分子结构
CAS号：154-42-7
6-Thioguanine/6-硫鸟嘌呤 化学结构 CAS号：154-42-7
6-Thioguanine/6-硫鸟嘌呤 3D分子结构 CAS号：154-42-7
规格 价格 会员价 库存 数量
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6-Thioguanine/6-硫鸟嘌呤 纯度/质量文件 产品仅供科研

货号：A393548 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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产品名称 DNA Methyltransferase ↓ 其他靶点 纯度
6-Thioguanine ✔ 98%
Zebularine ✔ 98%
Procainamide HCl ✔ 99%
5-Azacytidine ✔ 95%
Decitabine ✔ 99%
SGI-1027 ++

DNMT3A, IC50: 7.5 μM

DNMT1, IC50: 6 μM

 		99%+
RG108 +++

DNA methyltransferase, IC50: 115 nM

 		99%+
Guadecitabine sodium ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

6-Thioguanine/6-硫鸟嘌呤 生物活性

靶点

  • DNA Methyltransferase
描述 The DNA methyltransferase (DNMT) family are enzymes that can catalyze the transfer of methyl group to DNA using S-adenosylmethionine (SAM) as a methyl donor with subsequent conversion of SAM to S-adenosylhomocysteine (SAH). Inhibiting the DNMTs have shown particular promise in the treatment of haematological malignancies[1]. Thioguanine which is used for the therapy of acute leukemia could inhibit the DNMT1.
On both canine large T cell leukemia line CLGL-90 and B cell line CLL 17-7, after incubating with thioguanine at 1.5, 3.0 and 6.0 μM for 24 hours, DNMT1 expression measured was reduced. Global methylation also demonstrated significant decreases following treatment of 6.0 μM thioguanine[2]. Similar results could be seen on Jurkat T cells. When the cells were treated with 1 - 3 μM of thioguanine for 24 hours, the percentage of cytosine methylation showed a decrease from 3.92% to 3.39% with 3 μM of thioguanine[3].
In VC8 cells injected CD1 nude mice cancer model, 1.5 mg/kg of thioguanine was administered i.p. daily for ten days. The tumor growth was significantly delayed after the treatment of thioguanine[4].
作用机制 After exposing to thioguanine, the DNMT1 is shifted toward ubiquination-mediated proteasomal degradation via alteration of the expression of histone lysine-specific demethylase[2].

6-Thioguanine/6-硫鸟嘌呤 细胞实验

Cell Line
Concentration Treated Time Description References
Jurkat T cells 3 µM 24 hours Measure the replacement rate of SG in DNA, results showed approximately 10% of guanine was replaced with SG Anal Chem. 2010 Jul 1;82(13):5797-803.
HL-60 cells 3 µM 24 hours Measure the replacement rate of SG in DNA, results showed approximately 7.4% of guanine was replaced with SG Anal Chem. 2010 Jul 1;82(13):5797-803.
CCRF-CEM cells 3 µM 24 hours Measure the replacement rate of SG in DNA, results showed approximately 7% of guanine was replaced with SG Anal Chem. 2010 Jul 1;82(13):5797-803.
K-562 cells 3 µM 24 hours Measure the replacement rate of SG in DNA, results showed approximately 3% of guanine was replaced with SG Anal Chem. 2010 Jul 1;82(13):5797-803.
HCT-116 cells 3 µM 24 hours Measure the replacement rate of SG in DNA, results showed approximately 0.2% of guanine was replaced with SG Anal Chem. 2010 Jul 1;82(13):5797-803.
HEK293T cells 3.6 µM (EC50) 48 hours Evaluate the antiproliferative activity of 6-TG, results show HEK293T cells are highly sensitive to 6-TG J Med Chem. 2022 Nov 24;65(22):15165-15173.
K-562 cells 0.7 µM (EC50) 48 hours Evaluate the antiproliferative activity of 6-TG on K-562 cells, results show K-562 cells are sensitive to 6-TG J Med Chem. 2022 Nov 24;65(22):15165-15173.
THP-1 cells 0.3 µM (EC50) 48 hours Evaluate the antiproliferative activity of 6-TG on THP-1 cells, results show THP-1 cells are sensitive to 6-TG J Med Chem. 2022 Nov 24;65(22):15165-15173.
HCT116 cells 150 nM 72 hours To investigate the effect of NUDT15 knockdown on 6-TG-induced checkpoint activation, results showed that NUDT15 knockdown significantly enhanced 6-TG-induced Chk1 and Chk2 phosphorylation Cancer Res. 2016 Sep 15;76(18):5501-11.

6-Thioguanine/6-硫鸟嘌呤 动物研究

Dose Mice: 5 mg/kg, 10 mg/kg[5] (i.p.)
Administration i.p.

6-Thioguanine/6-硫鸟嘌呤 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03334266 Obesity Infan... 展开 >>t Obesity Mother-Child Relations Dietary Habits Breast Feeding Physical Activity Childhood Obesity Feeding Behavior 收起 << Not Applicable Recruiting December 31, 2021 United States, Arizona ... 展开 >> Johns Hopkins Center for American Indian Health Recruiting Fort Defiance, Arizona, United States, 86504 Contact: Allison Barlow, PhD    410-955-6931    abarlow@jhu.edu    Contact: Nicole Neault, MPH    5057973309    nneault@jhu.edu    Johns Hopkins Center for American Indian Health Recruiting Whiteriver, Arizona, United States, 85941 Contact: Allison Barlow, PhD    410-955-6931    abarlow@jhu.edu    Contact: Nicole Neault, MPH    5057973309    nneault@jhu.edu    United States, New Mexico Johns Hopkins Center for American Indian Health Recruiting Shiprock, New Mexico, United States, 87420 Contact: Allison Barlow, PhD    410-955-6931    abarlow@jhu.edu    Contact: Nicole Neault, MPH    5057973309    nneault@jhu.edu 收起 <<
NCT02281799 Pancreatitis ... 展开 >>Inflammatory Bowel Diseases 收起 << Phase 4 Recruiting January 2019 Israel ... 展开 >> Shaare Zedek Recruiting Jerusalem, Israel, 91031 收起 <<
NCT02046694 Acute Lymphoblastic Leukemia (... 展开 >>ALL) 收起 << Early Phase 1 Recruiting September 2021 United States, Maryland ... 展开 >> Johns Hopkins Hospital Recruiting Baltimore, Maryland, United States, 21287 Principal Investigator: Colleen Annesley, MD          Sub-Investigator: Patrick A Brown, MD          United States, Texas Texas Children's Cancer and Hematology Centers Recruiting Houston, Texas, United States, 77030 Contact: Julie Brackett, MD    832-822-4242       Sub-Investigator: Edward Sisson, MD          Principal Investigator: Julie Brackett, MD          United States, Washington Seattle Children's Hospital Recruiting Seattle, Washington, United States, 98105 Contact: Colleen Annesley, MD          Principal Investigator: Colleen Annesley, MD 收起 <<

6-Thioguanine/6-硫鸟嘌呤 参考文献

[1]Hogarth LA, Redfern CP, et al. The effect of thiopurine drugs on DNA methylation in relation to TPMT expression. Biochem Pharmacol. 2008;76(8):1024-35.

[2]Flesner BK, Kumar SR, et al. 6-Thioguanine and zebularine down-regulate DNMT1 and globally demethylate canine malignant lymphoid cells. BMC Vet Res. 2014.

[3]Wang H, Wang Y. 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;48(10):2290-9.

[4]Issaeva N, Thomas HD, et al. 6-thioguanine selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance. Cancer Res. 2010;70(15):6268-76.

6-Thioguanine/6-硫鸟嘌呤 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.98mL

1.20mL

0.60mL

29.91mL

5.98mL

2.99mL

59.81mL

11.96mL

5.98mL

6-Thioguanine/6-硫鸟嘌呤 技术信息

CAS号154-42-7
分子式C5H5N5S
分子量 167.19
SMILES Code S=C1N=C(N)NC2=C1NC=N2
MDL No. MFCD02730136
别名 硫鸟嘌呤 ;Thioguanine; 2-Amino-6-purinethiol; 6Mercapto2aminopurine; 6HPurine6thione 2amino17dihydro (9CI); 6 Thioguanine; 6 Mercaptoguanine; 2Amino 6MP; WR1141; BW 5071; Tabloid; 6-TG; NSC 76504; NSC 752
运输蓝冰
InChI Key WYWHKKSPHMUBEB-UHFFFAOYSA-N
Pubchem ID 2723601
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature
溶解方案

DMSO: 9 mg/mL(53.83 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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

Tags: 6-Thioguanine | 154-42-7 | Thioguanine | 2-Amino-6-purinethiol | Anti-infection | Cell Cycle/DNA Damage | Epigenetics | Autophagy | Apoptosis | Metabolic Enzyme/Protease | SARS-CoV | Deubiquitinase | DNA Methyltransferase | Autophagy | Apoptosis | Endogenous Metabolite | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | 6-Thioguanine/6-硫鸟嘌呤 纯度/质量文件 | 6-Thioguanine/6-硫鸟嘌呤 亚型比较 | 6-Thioguanine/6-硫鸟嘌呤 生物活性 | 6-Thioguanine/6-硫鸟嘌呤 动物研究 | 6-Thioguanine/6-硫鸟嘌呤 临床数据 | 6-Thioguanine/6-硫鸟嘌呤 参考文献 | 6-Thioguanine/6-硫鸟嘌呤 实验方案 | 6-Thioguanine/6-硫鸟嘌呤 技术信息

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