INH1
Based on 1 publication(s) in Google Scholar
INH1 specifically disrupts the Hec1/Nek2 interaction via direct Hec1 binding. INH1 shows promising cancer inhibition activity both in vitro and in vivo.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.89%
- No. CAS: 313553-47-8
- Fòrmula: C18H16N2OS
- Peso molecular:308.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) INH1
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Actividad biológica
Descripciòn
IC50 & Target
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NEK2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
8.8 μM
Compound: INH1
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Cytotoxicity against human HeLa cells after 4 days by XTT assay
Cytotoxicity against human HeLa cells after 4 days by XTT assay
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[PMID: 19243176] |
| K562 | IC50 |
11.7 μM
Compound: INH1
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Cytotoxicity against human K562 cells after 4 days by XTT assay
Cytotoxicity against human K562 cells after 4 days by XTT assay
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[PMID: 19243176] |
| MDA-MB-231 | IC50 |
0.839 μM
Compound: 3o
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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
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[PMID: 23526571] |
| MDA-MB-231 | IC50 |
8.6 μM
Compound: INH1
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Cytotoxicity against human MDA-MB-231 cells after 4 days XTT assay
Cytotoxicity against human MDA-MB-231 cells after 4 days XTT assay
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[PMID: 19243176] |
| MDA-MB-468 | IC50 |
10.5 μM
Compound: INH1
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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
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[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.
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Cell Line:MCF10A cells.
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Concentration:10 μM.
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Incubation Time:12 days.
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Result:Effectively inhibits the proliferation of human breast cancer lines.
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Cell Line:MCF10A cells.
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Concentration:25 μM.
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Incubation Time:24 h.
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Result:Nek2 reduction in INH1-treated cells may be independent of Hec1.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Xenografted nude mice breast cancer model[1].
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Dosage:50 or 100 mg/kg.
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Administration:I.P., every other day/25 cycles.
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Result:Inhibited tumor growth.
Chemical Information
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No. CAS 313553-47-8
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Appearance Solid
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Peso molecular 308.40
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Fòrmula C18H16N2OS
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Color White to off-white
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SMILES
O=C(NC1=NC(C2=CC=C(C)C=C2C)=CS1)C3=CC=CC=C3
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Synonyms
IBT13131
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
Add each solvent one by one: 17% Solutol HS-15 in Saline
Solubility: 20 mg/mL (64.85 mM); Suspended solution; Need ultrasonic
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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 | 3.2425 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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