Home Cytoskeletal Signaling Microtubule Associated inhibitor INH1 For research use only.

INH1

Synonyms: IBT 13131

INH1 (IBT 13131) is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction.

INH1 Chemical Structure

INH1 Chemical Structure

CAS No. 313553-47-8

Purity & Quality Control

Batch: S749301 DMSO]61 mg/mL]false]Ethanol]61 mg/mL]false]Water]Insoluble]false Purity: 99.65%
99.65

INH1 Related Products

Signaling Pathway

Microtubule Associated Signaling Pathways

Microtubule Associated Signaling Pathway

Biological Activity

Description INH1 (IBT 13131) is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction.
Targets
Hec1 [1]
In vitro
In vitro 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. [1]
Kinase Assay Binding assays
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 Research Cell lines MDA-MB-468, SKBR3, T47D, MDA-MB-361, ZR-75-1, HBL100, MDA-MB-435, HS578T, and MCF10A cells.
Concentrations ~50 μM
Incubation Time 3 days
Method 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.
In Vivo
In vivo INH1 (100 mg/kg i.p.) inhibits breast tumor growth in mice bearing MDA-MB-468 human breast cancer xenograft. [1]
Animal Research Animal Models Athymic female BALB/c nude mice bearing MDA-MB-468 human breast cancer xenografts.
Dosages ~100 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 308.40 Formula

C18H16N2OS
CAS No. 313553-47-8 SDF Download INH1 SDF
Smiles CC1=CC(=C(C=C1)C2=CSC(=N2)NC(=O)C3=CC=CC=C3)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 61 mg/mL ( (197.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 61 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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