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INH6

Catalog No.
B4757
Hec1/Nek2 inhibitor, potent
Grouped product items
SizePriceStock Qty
10mg
$55.00
In stock
50mg
$175.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

INH6 is a potent inhibitor of Hec1/Nek2 [1].

Hec1 is an oncogene that involved in spindle checkpoint signaling and is overexpressed in many human cancers. Nek2 is a serine/threonine-protein kinase that phosphorylates Hec1, which is critical for its mitotic function and cell survival [1].

INH6 is a potent Hec1/Nek2 inhibitor. INH6 inhibited Hec1/Nek2 function through protein degradation that led to chromosome mis-segregation and cell death. In MDA-MB468 and MDA-MB231 human breast cancer cell lines, HeLa human cervical cancer line and K562 human erythromyeloblastoid leukemia cell line, INH6 exhibited significantly anti-proliferation activities with IC50 values of 2.1, 1.7, 2.4 and 2.5 µM, respectively. In HeLa cell extract, INH6-conjugated matrix selectively co-precipitated with cellular Hec1, which suggested that INH6 bound to cellular Hec1. In Hela cells, INH6 (6.25 µM) reduced Nek2 by 50% at 8-11 h. In addition, INH6 slightly reduced Hec1 over time. Also, INH6 increased mitotic population with multipolar spindle configurations. In HeLa cells expressing the chromosome marker protein H2B-GFP, INH6 increased chromosome misalignment. In HeLa cells, INH6 exhibited progressive morphological changes of dying cells and induced apoptosis by 20% [1].

Reference:
[1].  Qiu XL, Li G, Wu G, et al. Synthesis and biological evaluation of a series of novel inhibitor of Nek2/Hec1 analogues. J Med Chem, 2009, 52(6): 1757-1767.

Chemical Properties

StorageDesiccate at -20°C
M.Wt322.42
Cas No.1001753-24-7
FormulaC19H18N2OS
Solubility≥32.2 mg/mL in DMSO; insoluble in H2O; ≥3.55 mg/mL in EtOH with gentle warming and ultrasonic
SDFDownload SDF
Canonical SMILESO=C(C1=CC=CC=C1)NC2=NC(C3=C(C)C=C(C)C=C3C)=CS2
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description INH6 is a potent inhibitor of Hec1
Targets Hec1/Nek2 complex          
IC50            

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