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Merck

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.

Synonym(s):

Hec1/Nek2 Mitotic Pathway Inhibitor II, INH6, N-(4-(2,4,6-Trimethylphenyl)-thiazol-2-yl)-benzamide, INH6

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About This Item

Empirical Formula (Hill Notation):
C19H18N2OS
CAS Number:
1001753-24-7
Molecular Weight:
322.42
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light

Key Documents

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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

storage temp.

2-8°C

Quality Level

100

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)

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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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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