N-(4-Mesitylthiazol-2-yl)benzaMide Chemical Properties

Melting point:

192-193 °C

Density 

1.216±0.06 g/cm3(Predicted)

storage temp. 

Desiccate at -20°C

solubility 

≥32.2 mg/mL in DMSO; insoluble in H2O; ≥3.55 mg/mL in EtOH with gentle warming and ultrasonic

form 

Powder

pka

7.07±0.70(Predicted)

color 

White to off-white

CAS DataBase Reference

1001753-24-7

N-(4-Mesitylthiazol-2-yl)benzaMide Usage And Synthesis

Uses

INH6 is a Hec1 inhibitor that targets the Hec1/Nek2 pathway and causes chromosome mis-alignment as well as cell death.

Biological Activity

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].

target

Hec1/Nek2 complex

References

[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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