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
InChI key
WCZLNJTXHZPHLM-UHFFFAOYSA-N
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)
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 100 mg/mL, ethanol: 5 mg/mL
shipped in
ambient
Quality Level
General description
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.
Packaging
Packaged under inert gas
Preparation Note
Following resonstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Qiu, X.L., et al. 2009. J. Med. Chem.52, 1757.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_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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