373271
Hec1/Nek2 Mitotic Pathway Inhibitor II, INH6
The Hec1/Nek2 Mitotic Pathway Inhibitor II, INH6, also referenced under CAS 1001753-24-7, controls the biological activity of Hec1/Nek2 Mitotic Pathway.
别名:
Hec1/Nek2 Mitotic Pathway Inhibitor II, INH6, N-(4-(2,4,6-Trimethylphenyl)-thiazol-2-yl)-benzamide, INH6
质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white
溶解性
DMSO: 100 mg/mL
ethanol: 5 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C19H18N2OS/c1-12-9-13(2)17(14(3)10-12)16-11-23-19(20-16)21-18(22)15-7-5-4-6-8-15/h4-11H,1-3H3,(H,20,21,22)
InChI key
WCZLNJTXHZPHLM-UHFFFAOYSA-N
一般描述
A cell-permeable INH1 (Cat. No. 373270) analog that contains a tri-, instead of di-, methylated aryl ring and exhibits significantly improved antiproliferative activity against MB231, MB468, HeLa, and K562 cells (IC50 = 1.7, 2.1, 2.4, and 2.5 µM, respectively) than INH1 (IC50 = 8.6, 10.5, 8.8, and 11.7 µM, respectively). Immobilized INH6 is shown to selectively pull down Hec1, but not Nek2, from HeLa cell extract. Treatment of HeLa cultures results in down-regulations of cellular Nek2 (6.25 µM , >4 h) and Hec1 (6.25 µM , >16 h), an increase in apoptotic G1 population (by 10-fold; 2.5 µM, 72 h), as well as increased mitotic abnormalities, including multipolar spindle formations and metaphase chromosome misalignment.
A cell-permeable INH1 (Cat. No. 373270) analog that contains a tri-, instead of di-, methylated aryl ring and exhibits significantly improved antiproliferative activity against MB231, MB468, HeLa, and K562 cells (IC50 = 1.7, 2.1, 2.4, and 2.5 µM, respectively) than INH1 (IC50 = 8.6, 10.5, 8.8, and 11.7 µM, respectively). Immobilized INH6 is shown to selectively pull down Hec1, but not Nek2, from HeLa cell extract. Treatment of HeLa cultures results in down-regulations of cellular Nek2 (6.25 µM, >4 h) and Hec1 (6.25 µM, >16 h), an increase in apoptotic G1 population (by 10-fold; 2.5 µM, 72 h), as well as increased mitotic abnormalities, including multipolar spindle formations and metaphase chromosome misalignment.
包装
Packaged under inert gas
制备说明
Following resonstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Qiu, X.L., et al. 2009. J. Med. Chem.52, 1757.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Yainyrette Rivera-Rivera et al.
Scientific reports, 11(1), 9016-9016 (2021-04-29)
Nek2 (NIMA-related kinase 2) is a serine/threonine-protein kinase that localizes to centrosomes and kinetochores, controlling centrosome separation, chromosome attachments to kinetochores, and the spindle assembly checkpoint. These processes prevent centrosome amplification (CA), mitotic dysfunction, and chromosome instability (CIN). Our group
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