INH1

INH1, a thiazolyl benzamide compound, is a cell-permeable Hec1/Nek2 mitotic pathway inhibitor I.

INH1
Names
Preferred IUPAC name
N-[4-(2,4-Dimethylphenyl)-1,3-thiazol-2-yl]benzamide
Identifiers
3D model (JSmol)
ChemSpider
  • InChI=1S/C18H16N2OS/c1-12-8-9-15(13(2)10-12)16-11-22-18(19-16)20-17(21)14-6-4-3-5-7-14/h3-11H,1-2H3,(H,19,20,21)
    Key: JPMOKRWIYQGMJL-UHFFFAOYSA-N
  • InChI=1/C18H16N2OS/c1-12-8-9-15(13(2)10-12)16-11-22-18(19-16)20-17(21)14-6-4-3-5-7-14/h3-11H,1-2H3,(H,19,20,21)
    Key: JPMOKRWIYQGMJL-UHFFFAOYAG
  • CC1=CC(=C(C=C1)C2=CSC(=N2)NC(=O)C3=CC=CC=C3)C
Properties
C18H16N2OS
Molar mass 308.40 g·mol−1
Density 1.2±0.1 g/cm3
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

Biological activity

INH1 controls the biological activity of Hec1/Nek2 mitotic pathway. It specifically disrupts the Hec1/Nek2 interaction[1] by directly binding to Hec1, resulting in defective Hec1 kinetochores localization and low-level cellular Nek2 protein. INH1 induces a transient mitotic arrest, exhibiting metaphase chromosome misalignment, spindle abnormality, and consequently cancer cell apoptosis.

Experiments show that INH1 potently inhibits the proliferation of multiple human breast cancer cell lines, cervical HeLa cells, and colon cancer cells in vitro.[2]

References
  1. "biological activity of INH1 by selleckchemicals". selleck.
  2. Wu G, et al. (Oct 15, 2008). "Small molecule targeting the Hec1/Nek2 mitotic pathway suppresses tumor cell growth in culture and in animal". Cancer Res. 68 (20): 8393–8399. doi:10.1158/0008-5472.can-08-1915. PMC 2709694. PMID 18922912.
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