product name INH1
Description: INH1 (also known as IBT 13131) is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction. 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.
References: Cancer Res. 2008 Oct 15;68(20):8393-9.
308.40
Formula
C18H16N2OS
CAS No.
313553-47-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 61 mg/mL (197.8 mM)
Water: <1 mg/mL
Ethanol: 61 mg/mL (197.8 mM)
Solubility (In vivo)
Synonyms
IBT 13131
other peoduct :
| In Vitro |
In vitro activity: INH1 reduces the association of Hec1 with kinetochore and decreases global Nek2 protein level in cells. INH1 effectively inhibits the proliferation of human breast cancer lines with GI50 of 10-21 μM. Moreover, INH1 also elicits cell killing activity in part through impairing the Hec1/Nek2 pathway for the spindle checkpoint regulation. Kinase Assay: Surface plasma resonance (SPR) assays are performed at 22.5°C in HBSD buffer [10 mmol/L HEPES, 150 mmol/L NaCl, 0.1% DMSO (pH 7.5)] on Biacore 3000. 6×His-Hec1 and GST-Nek2 are purified. NTA sensor chip or glutathione-modified CM5 chip are used to capture His-Hec1 and GST-Nek2, respectively. The capture level is about 140 to 180 resonance units (RU) at the flow rate of 5 μL/min. For the binding assay, chips are sequentially treated with compounds (1 or 20 μmol/L) and then proteins (50 μg/mL). Retained RUs are recorded and processed (triplicate experiments). Cell Assay: Standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays with a 3-d drug treatment procedure are performed to measure the dose-dependent cytotoxicity of INH1 in cultured cells. Triplicate sets are measured and compiled for final data presentation. Cell lines used: MDA-MB-468, SKBR3, T47D, MDA-MB-361, ZR-75-1, HBL100, MDA-MB-435, HS578T, and MCF10A cells. |
|---|---|
| In Vivo | INH1 (100 mg/kg i.p.) inhibits breast tumor growth in mice bearing MDA-MB-468 human breast cancer xenograft. |
| Animal model | Athymic female BALB/c nude mice bearing MDA-MB-468 human breast cancer xenografts. |
| Formulation & Dosage | Dissolved in 15% DMSO, 20% Tween 20, 10% PEG-400, 55% saline; 100 mg/kg; i.p. injection |
| References | Cancer Res. 2008 Oct 15;68(20):8393-9. |
