Home Cytoskeletal Signaling Microtubule Associated inhibitor INH1

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INH1 Microtubule Associated inhibitor

Cat.No.S7493

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

Chemical Structure

Molecular Weight: 308.40

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 308.40 Formula

C18H16N2OS

 Storage (From the date of receipt)
CAS No. 313553-47-8 Download SDF Storage of Stock Solutions

Synonyms IBT 13131 Smiles CC1=CC(=C(C=C1)C2=CSC(=N2)NC(=O)C3=CC=CC=C3)C

Solubility

In vitro
Batch:

DMSO : 61 mg/mL (197.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 61 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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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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Mechanism of Action

Targets/IC50/Ki
Hec1 [1]
In vitro
INH1 reduces the association of Hec1 with kinetochore and decreases global Nek2 protein level in cells. This compound effectively inhibits the proliferation of human breast cancer lines with GI50 of 10-21 μM. Moreover, it 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 this compound (1 or 20 μmol/L) and then proteins (50 μg/mL). Retained RUs are recorded and processed (triplicate experiments).
In vivo
INH1 (100 mg/kg i.p.) inhibits breast tumor growth in mice bearing MDA-MB-468 human breast cancer xenograft. [1]
References

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