Tioxolone, a metalloenzyme carbonic anhydrase I inhibitor with a Ki of 91 nM, is an anti-acne preparation.
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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 | 98% | ||||||||||||||||
Dichlorphenamide | ✔ | 98% | |||||||||||||||||
Mafenide Acetate | ✔ | 98% | |||||||||||||||||
Benzenesulphonamide | ✔ | 98% | |||||||||||||||||
Dorzolamide HCl |
+
Carbonic anhydrase I, Ki: 6000 nM |
++++
Carbonic anhydrase II, Ki: 1.9 nM |
+++
Carbonic anhydrase IV, Ki: 31 nM |
98% | |||||||||||||||
Methazolamide |
++
hCAI, Ki: 50 nM |
+++
hCAII, Ki: 14 nM |
++
bCAIV, Ki: 36 nM |
98% | |||||||||||||||
Tioxolone |
+
CAI, Ki: 91 nM |
98% | |||||||||||||||||
U-104 |
++
CAIX, Ki: 45.1 nM |
++++
CAXII, Ki: 4.5 nM |
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。 |
靶点 |
|
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]. |
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 |
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 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
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 |