INH1

Catalog No.S7493 Batch:S749301

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Technical Data

Formula

C18H16N2OS
Molecular Weight 308.40 CAS No. 313553-47-8
Solubility (25°C)* In vitro DMSO 61 mg/mL (197.79 mM)
Ethanol 61 mg/mL (197.79 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.75mg/ml
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description INH1 (IBT 13131) is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction.
Targets
Hec1 [1]
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]
In vivo INH1 (100 mg/kg i.p.) inhibits breast tumor growth in mice bearing MDA-MB-468 human breast cancer xenograft. [1]

Protocol (from reference)

Kinase Assay:[1]
  • 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 Assay:[1]
  • 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.
Animal Study:[1]
  • Animal Models

    Athymic female BALB/c nude mice bearing MDA-MB-468 human breast cancer xenografts.

  • Dosages

    ~100 mg/kg

  • Administration

    i.p.

Selleck's INH1 has been cited by 1 publication

Destabilizing NEK2 overcomes resistance to proteasome inhibition in multiple myeloma [ J Clin Invest, 2018, 128(7):2877-2893] PubMed: 29863498

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.