产品说明书

Tioxolone

Print
Chemical Structure| 4991-65-5 同义名 : Thioxolone
CAS号 : 4991-65-5
货号 : A436967
分子式 : C7H4O3S
纯度 : 98%
分子量 : 168.17
MDL号 : MFCD00005859
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：
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].
实验方案
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
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