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/ 6-Thioguanine

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

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

6-Thioguanine belongs to the thiopurine family of drugs that also include mercaptopurine and azathioprine, which are examples of antimetabolites, and is a purine analogue of the nucleobase guanine. It was found to inhibit SARS-CoV PLpro. 6-Thioguanine disrupts cytosine methylation by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo.

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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 化学结构 CAS号：154-42-7
6-Thioguanine 化学结构
CAS号：154-42-7
6-Thioguanine 3D分子结构
CAS号：154-42-7
6-Thioguanine 化学结构 CAS号：154-42-7
6-Thioguanine 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 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:

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产品名称 DNA Methyltransferase ↓ 其他靶点 纯度
6-Thioguanine ✔ 98%
Zebularine ✔ 98%
Procainamide hydrochloride ✔ 99%
5-Azacytidine ✔ 95%
Decitabine ✔ 99%
SGI-1027 ++

DNMT1, IC50: 6 μM

DNMT3A, IC50: 7.5 μM

 		99%+
RG108 +++

DNA methyltransferase, IC50: 115 nM

 		99%+
Guadecitabine sodium ✔ 99+%
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 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 动物研究

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

6-Thioguanine 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 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 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 技术信息

CAS号154-42-7
分子式C5H5N5S
分子量 167.192
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
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
溶解度

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
动物实验配方

IP 3% DMSO+3% Tween80+30% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 61 mg/mL suspension

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 纯度/质量文件 | 6-Thioguanine 亚型比较 | 6-Thioguanine 生物活性 | 6-Thioguanine 动物研究 | 6-Thioguanine 临床数据 | 6-Thioguanine 参考文献 | 6-Thioguanine 实验方案 | 6-Thioguanine 技术信息

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