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2-Thiouracil

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Chemical Structure| 141-90-2 同义名 : 硫代由雪 ;Thiouracil;Antagothyroil;NSC 290414;NSC 290413;NSC 290412;NSC 19473
CAS号 : 141-90-2
货号 : A399147
分子式 : C4H4N2OS
纯度 : 97%
分子量 : 128.152
MDL号 : MFCD00006039
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(390.16 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

动物实验配方:
生物活性
描述 2-Thiouracil (Thiouracil) is an antithyroid compound. 2-Thiouracil is a selective inhibitor of neuronal nitric oxide synthase (nNOS) with a Ki of 20 μM. The drug apparently interfered with the substrate- and tetrahydrobiopterin (BH(4))-binding to the enzyme. It caused a 60% inhibition of H(2)O(2) production in the absence of L-arginine and BH(4), and antagonised BH(4)-induced dimerisation of nNOS, but did not affect cytochrome c reduction[3]. 2-thiouridine (alone or within an RNA chain) is predominantly transformed under oxidative stress conditions to 4-pyrimidinone riboside (H2U) and not to uridine. 2-Thiouracil-containing nucleosides are essential modified units of natural and synthetic nucleic acids[4]. 2-thiouracil could not inhibit the synthesis of TMV (tobacco mosaic virus) RNA, but could inhibit some early functions of TMV. 1 mM 2-thiouracil inhibited viral protein and RNA synthesis totally when treatment began within the first 4 h after initiation of replication, but not at all when treatment began at 12 h or later[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

7.80mL

1.56mL

0.78mL

39.02mL

7.80mL

3.90mL

78.03mL

15.61mL

7.80mL

参考文献

[1]Palumbo A, d'Ischia M, Cioffi FA. 2-thiouracil is a selective inhibitor of neuronal nitric oxide synthase antagonising tetrahydrobiopterin-dependent enzyme activation and dimerisation. FEBS Lett. 2000 Nov 24;485(2-3):109-12.

[2]Napolitano A, Palumbo A, et al. Mechanism of selective incorporation of the melanoma seeker 2-thiouracil into growing melanin. J Med Chem. 1996 Dec 20;39(26):5192-201.

[3]Palumbo A, d'Ischia M, Cioffi FA. 2-thiouracil is a selective inhibitor of neuronal nitric oxide synthase antagonising tetrahydrobiopterin-dependent enzyme activation and dimerisation. FEBS Lett. 2000 Nov 24;485(2-3):109-12

[4]Sochacka E, Szczepanowski RH, Cypryk M, Sobczak M, Janicka M, Kraszewska K, Bartos P, Chwialkowska A, Nawrot B. 2-Thiouracil deprived of thiocarbonyl function preferentially base pairs with guanine rather than adenine in RNA and DNA duplexes. Nucleic Acids Res. 2015 Mar 11;43(5):2499-512

[5]Dawson WO, Grantham GL. Effect of 2-thiouracil on RNA and protein synthesis in synchronous and asynchronous infections of tobacco mosaic virus. Intervirology. 1983;19(3):155-61