JAK2-IN-6

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。

JAK2-IN-6 

JAK2-IN-6 是一种多取代的氨基噻唑衍生物,是一种有效的选择性 JAK2 抑制剂,IC50 为 22.86 μg/mL。JAK2-IN-6 对 JAK1 和 JAK3 没有活性,对癌细胞具有抗增殖作用。

JAK2-IN-6

JAK2-IN-6 Chemical Structure

CAS No. : 353512-04-6

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生物活性

JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells[1].

IC50 & Target[1]

JAK2

22.86 μg/mL (IC50)

体外研究
(In Vitro)

JAK2-IN-6 (Compound B2; 6.3-50 μg/mL; 48 hours; PC-9, H1975 and PANC-1 cells) treatment exhibits significantly antiproliferative activity against all of these cancer cell lines, with IC50 values of 18.1 μg/mL, 58.3 μg/mL, 40.6 μg/mL against PC-9, H1975 and PANC-1, respectively[1].
JAK2-IN-6 (Compound B2), an intramolecular hydrogen bond is formed, holding the chlorothiophene substituent coplanar with the aminothiazole core. The chlorothiophene moiety is found to be located in the binding pocket adjacent to Val863 and Leu983, and extends towards the Asp994 of activation loop and the Gly993 of glycine-rich loop[1].

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

Cell Proliferation Assay[1]

Cell Line: PC-9, H1975 and PANC-1 cells
Concentration: 6.3 μg/mL, 12.5 μg/mL, 25 μg/mL, 50 μg/mL
Incubation Time: 48 hours
Result: Exhibited significantly antiproliferative activity against all of these cancer cell lines.

分子量

335.83

Formula

C14H10ClN3OS2

CAS 号

353512-04-6

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]. Ting-Ting Yao, et al. Integration of pharmacophore mapping and molecular docking in sequential virtual screening: towards the discovery of novel JAK2 inhibitors. RSC Adv., 2017, 7, 10353-10360.

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