JH295
Based on 1 Customer Validation
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint. JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Purity: 98.66%
- CAS No.: 1311143-71-1
- 화학식: C18H16N4O2
- 분자량:320.35
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보관:
-20°C, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
Biological Activity
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NEK2 770 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1.3 μM
Compound: 16
|
Inhibition of hemagglutinin epitope-tagged human Nek2 transfected tetracycline-induced in human HEK293 cells pre-incubated for 45 mins by immunoprecipitation assay
Inhibition of hemagglutinin epitope-tagged human Nek2 transfected tetracycline-induced in human HEK293 cells pre-incubated for 45 mins by immunoprecipitation assay
|
[PMID: 21627121] |
JH295 (Compound 16; 0.08-20 μM; 45 minutes; RPMI7951 cells) treatment inhibits WT Nek2 in cells with an IC50 of ~1.3 μM, whereas it has little effect on the C22V mutant[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RPMI7951 cells
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Concentration:0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 6.6 μM, 20 μM
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Incubation Time:45 minutes
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Result:Inhibited WT Nek2 in cells with an IC50 of ~1.3 μM, whereas had little effect on the C22V mutant.
Chemical Information
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CAS No. 1311143-71-1
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Appearance Solid
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분자량 320.35
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화학식 C18H16N4O2
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Color Yellow to orange
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SMILES
C#CC(NC1=CC2=C(NC(/C2=C\C3=C(C)N=C(CC)N3)=O)C=C1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
용액&용해도
DMSO : 55 mg/mL (171.69 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. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1216 mL | 15.6079 mL | 31.2159 mL | 78.0396 mL |
| 5 mM | 0.6243 mL | 3.1216 mL | 6.2432 mL | 15.6079 mL | |
| 10 mM | 0.3122 mL | 1.5608 mL | 3.1216 mL | 7.8040 mL | |
| 15 mM | 0.2081 mL | 1.0405 mL | 2.0811 mL | 5.2026 mL | |
| 20 mM | 0.1561 mL | 0.7804 mL | 1.5608 mL | 3.9020 mL | |
| 25 mM | 0.1249 mL | 0.6243 mL | 1.2486 mL | 3.1216 mL | |
| 30 mM | 0.1041 mL | 0.5203 mL | 1.0405 mL | 2.6013 mL | |
| 40 mM | 0.0780 mL | 0.3902 mL | 0.7804 mL | 1.9510 mL | |
| 50 mM | 0.0624 mL | 0.3122 mL | 0.6243 mL | 1.5608 mL | |
| 60 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3007 mL | |
| 80 mM | 0.0390 mL | 0.1951 mL | 0.3902 mL | 0.9755 mL | |
| 100 mM | 0.0312 mL | 0.1561 mL | 0.3122 mL | 0.7804 mL |