INH6 |
Catalog No.GC10334
One-Click Copy Product Info
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INH6 est un puissant inhibiteur de Nek2/Hec1 ; inhibe la croissance des cellules HeLa avec une IC50 de 2,4 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1001753-24-7
Sample solution is provided at 25 µL, 10mM.
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INH6 is a potent inhibitor of Hec1/Nek2 [1].
Hec1 is an oncogene that involved in spindle checkpoint signaling and is overexpressed in many human cancers. Nek2 is a serine/threonine-protein kinase that phosphorylates Hec1, which is critical for its mitotic function and cell survival [1].
INH6 is a potent Hec1/Nek2 inhibitor. INH6 inhibited Hec1/Nek2 function through protein degradation that led to chromosome mis-segregation and cell death. In MDA-MB468 and MDA-MB231 human breast cancer cell lines, HeLa human cervical cancer line and K562 human erythromyeloblastoid leukemia cell line, INH6 exhibited significantly anti-proliferation activities with IC50 values of 2.1, 1.7, 2.4 and 2.5 µM, respectively. In HeLa cell extract, INH6-conjugated matrix selectively co-precipitated with cellular Hec1, which suggested that INH6 bound to cellular Hec1. In Hela cells, INH6 (6.25 µM) reduced Nek2 by 50% at 8-11 h. In addition, INH6 slightly reduced Hec1 over time. Also, INH6 increased mitotic population with multipolar spindle configurations. In HeLa cells expressing the chromosome marker protein H2B-GFP, INH6 increased chromosome misalignment. In HeLa cells, INH6 exhibited progressive morphological changes of dying cells and induced apoptosis by 20% [1].
Reference:
[1]. Qiu XL, Li G, Wu G, et al. Synthesis and biological evaluation of a series of novel inhibitor of Nek2/Hec1 analogues. J Med Chem, 2009, 52(6): 1757-1767.
Cell experiment: | 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]. |
References: [1]. Qiu XL, et al. Synthesis and biological evaluation of a series of novel inhibitor of Nek2/Hec1 analogues. J Med Chem. 2009 Mar 26;52(6):1757-67. | |
| Cas No. | 1001753-24-7 | SDF | |
| Canonical SMILES | O=C(C1=CC=CC=C1)NC2=NC(C3=C(C)C=C(C)C=C3C)=CS2 | ||
| Formula | C19H18N2OS | M.Wt | 322.42 |
| Solubility | ≥ 32.2mg/mL in DMSO | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1015 mL | 15.5077 mL | 31.0154 mL |
| 5 mM | 620.3 μL | 3.1015 mL | 6.2031 mL |
| 10 mM | 310.2 μL | 1.5508 mL | 3.1015 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)