1001753-24-7 Usage
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].
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1001753-24-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,0,1,7,5 and 3 respectively; the second part has 2 digits, 2 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1001753-24:
(9*1)+(8*0)+(7*0)+(6*1)+(5*7)+(4*5)+(3*3)+(2*2)+(1*4)=87
87 % 10 = 7
So 1001753-24-7 is a valid CAS Registry Number.
1001753-24-7Relevant articles and documents
Synthesis and biological evaluation of a series of novel inhibitor of Nek2/Hec1 analogues
Qui, Xiao-Long,Li, Guideng,Wu, Guikai,Zhu, Jiewen,Zhou, Longen,Chen, Phang-Lang,Chamberlin, A. Richard,Lee, Wen-Hwa
experimental part, p. 1757 - 1767 (2010/02/28)
High expression in cancer 1 (Hec1) is an oncogene overly expressed in many human cancers. Small molecule inhibitor of Nek2/Hec1 (INH) targeting the Hec1 and its regulator, Nek2, in the mitotic pathway, was identified to inactivate Hec1/Nek2 function media
