313553-47-8 Usage
Description
N-[4-(2,4-Dimethylphenyl)-2-thiazolyl]benzamidehydrochloride is a cell-permeable thiazolyl benzamide compound that directly binds to Hec1 and disrupts Hec1/Nek2 complex formation. This results in defective Hec1 kinetochores localization and cellular Nek2 destabilization/downregulation. It has been shown to induce a transient mitotic arrest in HeLa cultures and inhibit the proliferation of multiple human breast cancer cell lines in culture and in animal models.
Uses
Used in Pharmaceutical Industry:
N-[4-(2,4-Dimethylphenyl)-2-thiazolyl]benzamidehydrochloride is used as an anticancer agent for targeting the Hec1/Nek2 pathway. It effectively inhibits the proliferation of multiple human breast cancer cell lines, as well as the cervical HeLa and colon HCT116 cancer lines. It demonstrates reduced potency against the noncancerous MCF10A line, making it a promising candidate for cancer treatment.
Additionally, it has been reported to suppress tumor growth in a murine breast cancer model in vivo, indicating its potential use in cancer therapy.
Biological Activity
inh1 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 serine/threonine-protein kinase that phosphorylates hec1, which is critical for its mitotic function and cell survival [1].inh1 is a potent inhibitor of hec1/nek2 via directly binding to hec1. inh1 (1 and 20 μm) inhibited the ability of chip-immobilized hec1 binding to free nek2 by 39% and 55% but didn’t affect immobilized nek2 binding to free hec1, which suggested that inh1 directly bound to hec1. in the lysate from cells treated with inh1 (25 μm), the coimmunoprecipitate of hec1 with nek2 was inhibited, suggesting that inh1 disrupted the hec1/nek2 complex. inh1 (25 μm) significantly reduced cellular nek2 protein level by 80-90% in a time- and dose-dependent way and reduced kinetochore-bound hec1 pool by 55%. in human breast cancer cell lines, inh1 inhibited cell proliferation with gi50 values of 10-21 μm. in hela cells, inh1 increased the mitotic index by 2-fold and induced mitotic abnormalities [1].in nude mice xenografted breast cancer, inh1 inhibited tumor growth [1].
references
[1]. wu g, qiu xl, zhou l, et al. small molecule targeting the hec1/nek2 mitotic pathway suppresses tumor cell growth in culture and in animal. cancer res, 2008, 68(20): 8393-8399.
Check Digit Verification of cas no
The CAS Registry Mumber 313553-47-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,1,3,5,5 and 3 respectively; the second part has 2 digits, 4 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 313553-47:
(8*3)+(7*1)+(6*3)+(5*5)+(4*5)+(3*3)+(2*4)+(1*7)=118
118 % 10 = 8
So 313553-47-8 is a valid CAS Registry Number.
