S4 is a selective inhibitor of CA IX and CA XII inhibitor. The Ki values are 2, 7, 547 and 5600 nM for CA XII, IX, II and I, respectively.
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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。 |
描述 | CAIX Inhibitor S4 is a potent, selective inhibitor of CA IX/XII with Ki values of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki of 546 nM and 5600 nM, respectively). CAIX Inhibitor S4 inhibits orthotopic MDA-MB-231 mouse model of the number of lung metastases without affecting primary tumour growth. In the concentration range of 1-100 μM for 24 h, CAIX Inhibitor S4 inhibited the proliferation of MDA-MB-231, HCT116 and HT29 cells in a dose-dependent manner. While in the concentration range of 3.3-33 μM, CAIX Inhibitor S4 inhibited the migration of eGFP-MDA-MB-231 cells under hypoxia in a concentration-dependent manner. At a concentration of 33 μM for 15-60 minutes, CAIX Inhibitor S4 retarded the spreading of MDA-MB-231 cells in hypoxia, but essentially not in normoxia[1]. |
Animal study | At a dose of 10 mg/kg administered intraperitoneally for 14 days, CAIX Inhibitor S4 inhibited metastatic tumour load in the MDA-MB-231 model, but had no effect on primary tumour growth or the condition of the mice[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.98mL 0.60mL 0.30mL |
14.91mL 2.98mL 1.49mL |
29.82mL 5.96mL 2.98mL |
CAS号 | 1330061-67-0 |
分子式 | C15H17N3O4S |
分子量 | 335.378 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 250 mg/mL(745.43 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 |