Art. -Nr.: HY-16660

INH1

(Synonyms: IBT13131)

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INH1 specifically disrupts the Hec1/Nek2 interaction via direct Hec1 binding. INH1 shows promising cancer inhibition activity both in vitro and in vivo.

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Reinheit: 99.85%
CAS. Nr.: 313553-47-8
Formel: C₁₈H₁₆N₂OS
Molecular Weight:308.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

INH1 Chemical Structure

CAS. Nr.: 313553-47-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

INH1 specifically disrupts the Hec1/Nek2 interaction via direct Hec1 binding. INH1 shows promising cancer inhibition activity both in vitro and in vivo^[1].

IC₅₀ & Target

NEK2

Alle NEKs Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	8.8 μM Compound: INH1	Cytotoxicity against human HeLa cells after 4 days by XTT assay Cytotoxicity against human HeLa cells after 4 days by XTT assay	[PMID: 19243176]
K562	IC₅₀	11.7 μM Compound: INH1	Cytotoxicity against human K562 cells after 4 days by XTT assay Cytotoxicity against human K562 cells after 4 days by XTT assay	[PMID: 19243176]
MDA-MB-231	IC₅₀	0.839 μM Compound: 3o	Inhibition of cell migration in human MDA-MB-231 cells assessed as total number of cells after 24 hrs by transwell migration assay Inhibition of cell migration in human MDA-MB-231 cells assessed as total number of cells after 24 hrs by transwell migration assay	[PMID: 23526571]
MDA-MB-231	IC₅₀	8.6 μM Compound: INH1	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-468	IC₅₀	10.5 μM Compound: INH1	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]

In Vitro

INH1 (25 μM, 24 h) treatment resulted in reduced association of Hec1 with kinetochore and decrease of global Nek2 protein level^[1].
INH1 exhibits GI₅₀ values of 10.5 μM (in MDA-MB-468 cells), 15 μM (in SKBR3 cells), 10.5 μM (in T47D cells), 20.5 μM (in MDA-MB-361 cells), 15 μM (in ZR-75-1 cells), 15 μM (in HBL 100 cells), 15.5 μM (in MDA-MB-435 cells), 11 μM (in HS578T cells) and 41 μM (in MCF10A cells), respectively^[1].
INH1 (5k) has an IC₅₀ value of 176 nM in the dose-dependent transwell migration assays in MDA-MB-231 cells. INH1 (5k) substantially reduces cellular f-actin and prevented localization of fascin to actin-rich membrane protrusions^[2].
INH1 induces abnormal mitotic processes, as well as cell apoptosis^[3].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

MCF10A cells.
Concentration:

10 μM.
Incubation Time:

12 days.
Result:

Effectively inhibits the proliferation of human breast cancer lines.

Western Blot Analysis^[1]

Cell Line:

MCF10A cells.
Concentration:

25 μM.
Incubation Time:

24 h.
Result:

Nek2 reduction in INH1-treated cells may be independent of Hec1.

In Vivo

INH1 (50 or 100 mg/kg, i.p., every other day/25 cycles) inhibits tumor outgrowth in a xenografted breast cancer model in nude mice^[1].

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

Animal Model:

Xenografted nude mice breast cancer model^[1].
Dosage:

50 or 100 mg/kg.
Administration:

I.P., every other day/25 cycles.
Result:

Inhibited tumor growth.

Chemical Information

CAS. Nr. 313553-47-8
Appearance Solid
Molecular Weight 308.40
Formel C₁₈H₁₆N₂OS
Color White to off-white
SMILES

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

IBT13131
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (324.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2425 mL

16.2127 mL

32.4254 mL

5 mM

0.6485 mL

3.2425 mL

6.4851 mL

10 mM

0.3243 mL

1.6213 mL

3.2425 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 17% Solutol HS-15 in Saline

Solubility: 20 mg/mL (64.85 mM); Suspended solution; Need ultrasonic

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wu G, et al. Small molecule targeting the Hec1/Nek2 mitotic pathway suppresses tumor cell growth in culture and in animal. Cancer Res. 2008 Oct 15;68(20):8393-9. [Content Brief]

[2]. Shilong Zheng, et al. Discovery of a Series of Thiazole Derivatives as Novel Inhibitors of Metastatic Cancer Cell Migration and Invasion. ACS Med Chem Lett. 2013 Feb 14; 4(2): 191–196. [Content Brief]

[3]. Yongxia Zhu, et al. Small Molecule TH-39 Potentially Targets Hec1/Nek2 Interaction and Exhibits Antitumor Efficacy in K562 Cells via G0/G1 Cell Cycle Arrest and Apoptosis Induction. Cell Physiol Biochem. 2016;40(1-2):297-308. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	3.2425 mL	16.2127 mL	32.4254 mL	81.0636 mL
	5 mM	0.6485 mL	3.2425 mL	6.4851 mL	16.2127 mL
	10 mM	0.3243 mL	1.6213 mL	3.2425 mL	8.1064 mL
	15 mM	0.2162 mL	1.0808 mL	2.1617 mL	5.4042 mL
	20 mM	0.1621 mL	0.8106 mL	1.6213 mL	4.0532 mL
	25 mM	0.1297 mL	0.6485 mL	1.2970 mL	3.2425 mL
	30 mM	0.1081 mL	0.5404 mL	1.0808 mL	2.7021 mL
	40 mM	0.0811 mL	0.4053 mL	0.8106 mL	2.0266 mL
	50 mM	0.0649 mL	0.3243 mL	0.6485 mL	1.6213 mL
	60 mM	0.0540 mL	0.2702 mL	0.5404 mL	1.3511 mL
	80 mM	0.0405 mL	0.2027 mL	0.4053 mL	1.0133 mL
	100 mM	0.0324 mL	0.1621 mL	0.3243 mL	0.8106 mL

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INH1

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle NEKs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

INH1

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle NEKs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

INH1 Related Classifications

HY-16660 Related Classifications