INH6 (INH-6; INH 6) is a novel, potent and cell-permeable inhibitor of High expression in cancer 1 (Hec1) with potential anticancer activity. It specifically inhibits the Hec1-Nek2 protein-protein interactions disrupts, thus causing chromosome mis-alignment and cell death. INH6 shows potent anti-proliferative activity in vitro against various cancer cell lines such as MDA-MB468, MDA-MB231 human breast cancer cells, HeLa human cervical cancer line and K562 human erythromyeloblastoid leukemia cells with IC50 values of 2.1, 1.7, 2.4 and 2.5 µM, respectively.

Physicochemical Properties

Molecular Formula	C19H18N2OS
Molecular Weight	322.42
Exact Mass	322.113
CAS #	1001753-24-7
Related CAS #	1001753-24-7
PubChem CID	7918451
Appearance	White to off-white solid powder
Density	1.2±0.1 g/cm3
Index of Refraction	1.647
LogP	5.7
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	3
Heavy Atom Count	23
Complexity	398
Defined Atom Stereocenter Count	0
InChi Key	WCZLNJTXHZPHLM-UHFFFAOYSA-N
InChi Code	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)
Chemical Name	N-[4-(2,4,6-Trimethylphenyl)-1,3-thiazol-2-yl]benzamide
Synonyms	INH6; INH-6; INH 6
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	Many human cancers overexpress the oncogene Hec1. The mitotic pathway's Hec1/Nek2 function is inactivated by the small molecule INH (Inhibitor of Nek2/Hec1), which targets Hec1 and its regulator, Nek2. This process is mediated by protein degradation, which ultimately results in chromosome missegregation and cell death. Increased mitotic population and multipolar spindle configurations are seen in cells treated with INH6. After HeLa cells expressing the chromosome marker protein H2B-GFP are treated with INH6, a higher rate of chromosome misalignment is observed. INH6-treated cells exhibit progressive morphological changes indicative of dying cells, such as membrane bubbling, which are further supported by FACS analysis and cell cycle profiling. Seventy-two hours after treatment, 20% of INH6-treated cells undergo apoptosis[1].
ln Vivo
Animal Protocol
References	[1]. Synthesis and biological evaluation of a series of novel inhibitor of Nek2/Hec1 analogues. J Med Chem. 2009 Mar 26;52(6):1757-67.

Solubility Data

Solubility (In Vitro)

DMSO:64 mg/mL (198.5 mM) Water:<1 mg/mL Ethanol:11 mg/mL (34.1 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.1015 mL	15.5077 mL	31.0154 mL
	5 mM	0.6203 mL	3.1015 mL	6.2031 mL
	10 mM	0.3102 mL	1.5508 mL	3.1015 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.