INH6

Hec1/Nek2 inhibitor, potent CAS# 1001753-24-7

INH6

Catalog No. BCC5455----Order now to get a substantial discount!

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INH6: 5mg $35 In Stock
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Chemical structure

INH6

3D structure

Chemical Properties of INH6

Cas No. 1001753-24-7 SDF Download SDF
PubChem ID 7918451 Appearance Powder
Formula C19H18N2OS M.Wt 322.42
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 50 mg/mL (155.08 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name N-[4-(2,4,6-trimethylphenyl)-1,3-thiazol-2-yl]benzamide
SMILES CC1=CC(=C(C(=C1)C)C2=CSC(=N2)NC(=O)C3=CC=CC=C3)C
Standard InChIKey WCZLNJTXHZPHLM-UHFFFAOYSA-N
Standard InChI 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of INH6

DescriptionINH6 is a potent inhibitor of Hec1
TargetsHec1/Nek2 complex    

Protocol

Cell Assay [1]
Standard XTT assays with a four-day drug treatment procedure were performed to measure the dose-dependent cytotoxicity of INH analogs in cultured cells. Triplicate sets were measured and compiled for final data presentation. Cells were plated on 96-well dishes one day before the drug treatment, followed by drug treatment (2.5 μM INH6) on day 2 and XTT assay on day 5 after drug addition. The absorption at 595 nm was measured with a plate reader and converted to cell survival percentages in comparison to mock treated groups[1].

References:
[1]. Qiu XL, et al. Synthesis and biological evaluation of a series of novel inhibitor of Nek2/Hec1 analogues. J Med Chem. 2009 Mar 26;52(6):1757-67.

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Background on INH6

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.

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Description

INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC50 of 2.4 μM.

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