Carbonic anhydrase inhibitor 12

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Carbonic anhydrase inhibitor 12 

碳酸酐酶抑制剂12是一种有效的 CA II 抑制剂，对 CA I 也有抑制活性(CA II与CA I的 Kis分别为1.72 nM和271 nM)。碳酸酐酶抑制剂12对不同的肿瘤细胞系具有较强的抗癌活性。

Carbonic anhydrase inhibitor 12

Carbonic anhydrase inhibitor 12 Chemical Structure

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生物活性

Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines[1].

IC50 & Target

Ki: 1.72 nM (CA II), 271 nM (CA I)[1]
体外研究
(In Vitro)

Carbonic anhydrase inhibitor 12 (Compound 14h) (10 μM; 48 hours; single) has great influence on the specificity and the inhibitory potency against the different cancer cell lines[1].
Carbonic anhydrase inhibitor 12 (2.4 μM in MCF-7 and 2.5 μM MDA-MB-231; 48 hours) can arrest the cell cycle of MCF-7 and MDA-MB-231 cells at the G2/M phase[1].
Carbonic anhydrase inhibitor 12 (2.4 μM in MCF-7 and 2.5 μM MDA-MB-231; 48 hours) demonstrates an increase in the early apoptotic and late apoptotic phase in comparison to the control untreated cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: MCF-7, T47D, MDA-MB-231, COLO 205, HCT-116, HT29, SW-620, A549, SK-OV-3 and NCI-ADR-RES[1]
Concentration: 10 μM
Incubation Time: 48 hours
Result: Showed a mean growth inhibitory activity of 55.12% and a broad range of antiproliferative activity against most of the tested cancer cell lines.

Cell Cycle Analysis

Cell Line: MCF-7 and MDA-MB-231[1]
Concentration: 2.4 μM in MCF-7, 2.5 μM MDA-MB-231
Incubation Time: 48 hours
Result: Arrested the cell cycle of MCF-7 and MDA-MB-231 cells at the G2/M phase.

Apoptosis Analysis

Cell Line: MCF-7 and MDA-MB-231[1]
Concentration: 2.4 μM in MCF-7, 2.5 μM MDA-MB-231
Incubation Time: 48 hours
Result: Demonstrated an increase in the early apoptotic and late apoptotic phase in comparison to the control untreated cells.

分子量

640.53

Formula

C27H22BrN5O5S2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Abdel-Mohsen HT, et al. Application of the dual-tail approach for the design and synthesis of novel Thiopyrimidine-Benzenesulfonamide hybrids as selective carbonic anhydrase inhibitors. Eur J Med Chem. 2022;228:114004.

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