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噻克索酮 /Tioxolone {[allProObj[0].p_purity_real_show]}

货号:A436967 同义名: Thioxolone Ambeed 开学季,买赠积分,赢豪礼

Tioxolone, a metalloenzyme carbonic anhydrase I inhibitor with a Ki of 91 nM, is an anti-acne preparation.

Tioxolone 化学结构 CAS号:4991-65-5
Tioxolone 化学结构
CAS号:4991-65-5
Tioxolone 3D分子结构
CAS号:4991-65-5
Tioxolone 化学结构 CAS号:4991-65-5
Tioxolone 3D分子结构 CAS号:4991-65-5
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Tioxolone 纯度/质量文件 产品仅供科研

货号:A436967 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Carbonic Anhydrase Carbonic Anhydrase I Carbonic Anhydrase II Carbonic Anhydrase IV Carbonic Anhydrase IX Carbonic Anhydrase XII 其他靶点 纯度
Topiramate Calcium Channel {[allProObj[0].p_purity_real_show]}
Dichlorphenamide {[allProObj[0].p_purity_real_show]}
Mafenide Acetate {[allProObj[0].p_purity_real_show]}
Benzenesulphonamide {[allProObj[0].p_purity_real_show]}
Dorzolamide HCl +

Carbonic anhydrase I, Ki: 6000 nM

++++

Carbonic anhydrase II, Ki: 1.9 nM

+++

Carbonic anhydrase IV, Ki: 31 nM

{[allProObj[0].p_purity_real_show]}
Methazolamide ++

hCAI, Ki: 50 nM

+++

hCAII, Ki: 14 nM

++

bCAIV, Ki: 36 nM

{[allProObj[0].p_purity_real_show]}
Tioxolone +

CAI, Ki: 91 nM

{[allProObj[0].p_purity_real_show]}
U-104 ++

CAIX, Ki: 45.1 nM

++++

CAXII, Ki: 4.5 nM

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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。

Tioxolone 生物活性

靶点
  • Carbonic Anhydrase I

    CAI, Ki:91 nM

描述 Thioxolone is proposed to be a prodrug inhibitor that is cleaved via a CA II zinc-hydroxide mechanism known to catalyze the hydrolysis of esters[3]. Thioxolone acts as a prodrug in the presence of carbonic anhydrase II (CA II), whereby the molecule is cleaved by thioester hydrolysis to the carbonic anhydrase inhibitor, 4-mercaptobenzene-1,3-diol (TH0) [4]. Thioxolone was inefficient for generating isozyme-selective inhibitors, since except for CA I which is inhibited in the nanomolar range (K(I) of 91 nM), the remaining 12 isoforms were inhibited with a very flat profile (K(I)s in the range of only 4.93-9.04 microM) [5].

Tioxolone 参考文献

[1]Kim BH, Min YS, et al. Benzoxathiol derivative BOT-4-one suppresses L540 lymphoma cell survival and proliferation via inhibition of JAK3/STAT3 signaling. Exp Mol Med. 2011 May 31;43(5):313-21.

[2]Byres M, Cox PJ. The supramolecular structure of 6-hydroxy-1,3-benzoxathiol-2-one (tioxolone). Acta Crystallogr C. 2004 Jun;60(Pt 6):o395-6.

[3]Barrese AA 3rd, Genis C, Fisher SZ, Orwenyo JN, Kumara MT, Dutta SK, Phillips E, Kiddle JJ, Tu C, Silverman DN, Govindasamy L, Agbandje-McKenna M, McKenna R, Tripp BC. Inhibition of carbonic anhydrase II by thioxolone: a mechanistic and structural study. Biochemistry. 2008 Mar 11;47(10):3174-84

[4]Sippel KH, Genis C, Govindasamy L, Agbandje-McKenna M, Kiddle JJ, Tripp BC, McKenna R. Synchrotron Radiation Provides a Plausible Explanation for the Generation of a Free Radical Adduct of Thioxolone in Mutant Carbonic Anhydrase II. J Phys Chem Lett. 2010 Oct 7;1(19):2898-2902

[5]Innocenti A, Maresca A, Scozzafava A, Supuran CT. Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? Bioorg Med Chem Lett. 2008 Jul 15;18(14):3938-41

Tioxolone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.95mL

1.19mL

0.59mL

29.73mL

5.95mL

2.97mL

59.46mL

11.89mL

5.95mL

Tioxolone 技术信息

CAS号4991-65-5
分子式C7H4O3S
分子量 168.17
别名 Thioxolone
运输蓝冰
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: 105 mg/mL(624.37 mM),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
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