1. Cell Cycle/DNA Damage Apoptosis
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  3. INH6

INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC50 of 2.4 μM.

For research use only. We do not sell to patients.

INH6 Chemical Structure

INH6 Chemical Structure

CAS No. : 1001753-24-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 32 In-stock
10 mg USD 50 In-stock
25 mg USD 110 In-stock
50 mg USD 180 In-stock
100 mg USD 340 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC50 of 2.4 μM.

IC50 & Target

NEK2

 

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
2.4 μM
Compound: 6
Cytotoxicity against human HeLa cells after 4 days by XTT assay
Cytotoxicity against human HeLa cells after 4 days by XTT assay
[PMID: 19243176]
HeLa IC50
3.6 μM
Compound: 2
Antiproliferative activity against human HeLa cells assessed as cell viability after 96 hrs by CellTiter96 assay
Antiproliferative activity against human HeLa cells assessed as cell viability after 96 hrs by CellTiter96 assay
[PMID: 24773549]
K562 IC50
2.5 μM
Compound: 6
Cytotoxicity against human K562 cells after 4 days by XTT assay
Cytotoxicity against human K562 cells after 4 days by XTT assay
[PMID: 19243176]
K562 IC50
3.2 μM
Compound: 2
Antiproliferative activity against human K562 cells assessed as cell viability after 96 hrs by CellTiter96 assay
Antiproliferative activity against human K562 cells assessed as cell viability after 96 hrs by CellTiter96 assay
[PMID: 24773549]
MDA-MB-231 IC50
1.7 μM
Compound: 6
Cytotoxicity against human MDA-MB-231 cells after 4 days XTT assay
Cytotoxicity against human MDA-MB-231 cells after 4 days XTT assay
[PMID: 19243176]
MDA-MB-231 IC50
3.2 μM
Compound: 2
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 96 hrs by CellTiter96 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 96 hrs by CellTiter96 assay
[PMID: 24773549]
MDA-MB-468 IC50
2.1 μM
Compound: 6
Cytotoxicity against human MDA-MB-468 cells after 4 days by XTT assay
Cytotoxicity against human MDA-MB-468 cells after 4 days by XTT assay
[PMID: 19243176]
MDA-MB-468 IC50
2.2 μM
Compound: 2
Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 96 hrs by CellTiter96 assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 96 hrs by CellTiter96 assay
[PMID: 24773549]
In Vitro

Hec1 is an oncogene overly expressed in many human cancers. Small molecule INH (Inhibitor of Nek2/Hec1) targeting the Hec1 and its regulator, Nek2, in the mitotic pathway is identified to inactivate Hec1/Nek2 function mediated by protein degradation that subsequently leads to chromosome mis-segregation and cell death. INH6 treated cells exhibit increased mitotic population with multipolar spindle configurations. An increased rate of chromosome misalignment is detected upon treatment with INH6 of HeLa cells expressing the chromosome marker protein H2B-GFP. INH6 treated cells shows progressive morphological changes characteristic of dying cells (e.g., membrane bubbling), which is further confirmed by cell cycle profiling with FACS analysis. Approximately 20% of INH6 treated cells are apoptotic 72 hrs after treatment[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

322.42

Formula

C19H18N2OS

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=NC(C2=C(C)C=C(C)C=C2C)=CS1)C3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (155.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1015 mL 15.5077 mL 31.0154 mL
5 mM 0.6203 mL 3.1015 mL 6.2031 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Cell Assay
[1]

Standard XTT assays with a four-day drug treatment procedure were performed to measure the dose-dependent cytotoxicity of INH analogs in cultured cells. Triplicate sets were measured and compiled for final data presentation. Cells were plated on 96-well dishes one day before the drug treatment, followed by drug treatment (2.5 μM INH6) on day 2 and XTT assay on day 5 after drug addition. The absorption at 595 nm was measured with a plate reader and converted to cell survival percentages in comparison to mock treated groups[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1015 mL 15.5077 mL 31.0154 mL 77.5386 mL
5 mM 0.6203 mL 3.1015 mL 6.2031 mL 15.5077 mL
10 mM 0.3102 mL 1.5508 mL 3.1015 mL 7.7539 mL
15 mM 0.2068 mL 1.0338 mL 2.0677 mL 5.1692 mL
20 mM 0.1551 mL 0.7754 mL 1.5508 mL 3.8769 mL
25 mM 0.1241 mL 0.6203 mL 1.2406 mL 3.1015 mL
30 mM 0.1034 mL 0.5169 mL 1.0338 mL 2.5846 mL
40 mM 0.0775 mL 0.3877 mL 0.7754 mL 1.9385 mL
50 mM 0.0620 mL 0.3102 mL 0.6203 mL 1.5508 mL
60 mM 0.0517 mL 0.2585 mL 0.5169 mL 1.2923 mL
80 mM 0.0388 mL 0.1938 mL 0.3877 mL 0.9692 mL
100 mM 0.0310 mL 0.1551 mL 0.3102 mL 0.7754 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
INH6
Cat. No.:
HY-100541
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