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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:
Molecular Weight:
322.42
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

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

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

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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