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羟基脲 /Hydroxyurea {[allProObj[0].p_purity_real_show]}

货号:A145474 同义名: N-(氨基羰基)羟胺 / Hydroxycarbamide;NCI C04831

Hydroxyurea是一种细胞凋亡诱导剂,通过靶向核苷酸还原酶抑制 DNA 合成,还显示出抗正痘病毒活性。

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Type HazMat fee for 500 gram (Estimated)
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Inaccessible (Haz class 6.1), Domestic USD 80+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Hydroxyurea 化学结构 CAS号:127-07-1
Hydroxyurea 化学结构
CAS号:127-07-1
Hydroxyurea 3D分子结构
CAS号:127-07-1
Hydroxyurea 化学结构 CAS号:127-07-1
Hydroxyurea 3D分子结构 CAS号:127-07-1
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Hydroxyurea 纯度/质量文件 产品仅供科研

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产品名称 DNA synthesis helicase RdRp ribonucleotide reductase tRNA synthetase YB-1 其他靶点 纯度
Fexinidazole 98%
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Metronidazole 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
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Nedaplatin 99%+
Bendamustine 98+%
Trifluridine 98%
Robinetin 99%+
Carboplatin 99%
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Cisplatin 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

99%+
Oxaliplatin 98%
YK-4-279 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, IC50: 0.97 μM

99%+
RK-33 98%
Brr2-IN-3 99%+
Phen-DC3 Trifluoromethanesulfonate 98%
Favipiravir 97%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

97%
Didox 98%
(E)-3-AP 97%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, Kd: 42.1 nM

Leucyl-tRNA synthetase, IC50: 46.11 nM

98%
SU056 +

YB-1, IC50: 1.73 μM

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。

Hydroxyurea 生物活性

描述 Ribonucleotide reductase (RNR) is an emzyme that catalyses the rate limiting step in the production of deoxyribonucleotides needed for DNA synthesis[1]. RNR inhibitors are a family of anti-cancer drugs because they could affect the growth of tumor cells by interfering the DNA synthesis. Hydroxyurea (HU) is the inhibitor of ribonucleotide reductase (RNR) with IC50 value of 150 μM[2].
The ML L5178 cells, HU treatment at concentrations 0.25 mmol/l resulted in significant increases of DNA damage, detected as strand breaks in the alkaline comet assay [3]. After incubation with 2 mM HU for 4 hours on MCF7 cells, the level of phosphorylated RPA2 measured significantly increased and for 6 hours the percentage of cells with ssDNA was markedly decreased[4].
The pregnant C57BL/6 mice was intraperitoneally injected with 225 mg/kg HU and their embryos were explanted later. The RNR activity decreased significantly after 1 hour and the dNTP level in the brain tissues was attenuated with time[5].
作用机制 The HU is converted into its oxidized form compound III in the radical site of the ribonucleotide reductase protein. The compound III then reacts with the active site residues specially Tyr-176, and inhibits the radical generation and subsequently inhibits the RNR enzyme[6].

Hydroxyurea 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
L1210 Leukemia cells Growth inhibition assay Concentration required for 50% inhibition of cell growth (L1210 Leukemia), IC50=21.3796 μM 2991520
P388 leukemic cell Proliferation assay 24-48 h Antiproliferative activity of compound expressed as concentration that inhibits 50% of growth of P388 leukemic cell suspension from 24 to 48 hr after compound addition, IC50=32 μM 2709372

Hydroxyurea 动物研究

Dose Mice: 25 mg/kg - 100 mg/kg[7] (i.p.)
Administration i.p.

Hydroxyurea 参考文献

[1]Elledge SJ, Zhou Z, et al. Ribonucleotide reductase: regulation, regulation, regulation. Trends Biochem Sci. 1992;17(3):119-23.

[2]Tholander F, Sjöberg BM. Discovery of antimicrobial ribonucleotide reductase inhibitors by screening in microwell format. Proc Natl Acad Sci U S A. 2012;109(25):9798-803.

[3]Osterman Golkar S, Czene S, et al. Intracellular deoxyribonucleotide pool imbalance and DNA damage in cells treated with hydroxyurea, an inhibitor of ribonucleotide reductase. Mutagenesis. 2013;28(6):653-60.

[4]Shi W, Feng Z, et al. The role of RPA2 phosphorylation in homologous recombination in response to replication arrest. Carcinogenesis. 2010;31(6):994-1002.

[5]Guan Z, Wang X, et al. dNTP deficiency induced by HU via inhibiting ribonucleotide reductase affects neural tube development. Toxicology. 2015.

[6]Iman M, Khansefid Z, et al. Modeling and Proposed Molecular Mechanism of Hydroxyurea Through Docking and Molecular Dynamic Simulation to Curtail the Action of Ribonucleotide Reductase. Recent Pat Anticancer Drug Discov. 2016;11(4):461-468.

Hydroxyurea 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

13.15mL

2.63mL

1.31mL

65.75mL

13.15mL

6.57mL

131.49mL

26.30mL

13.15mL

Hydroxyurea 技术信息

CAS号127-07-1
分子式CH4N2O2
分子量 76.055
别名 N-(氨基羰基)羟胺 ;Hydroxycarbamide;NCI C04831;Droxia;Carbamoyl oxime;Biosupressin;NSC 32065
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: 50 mg/mL(657.42 mM),配合低频超声助溶,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

H2O: 50 mg/mL(657.42 mM),配合低频超声助溶

动物实验配方
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