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  3. JH295

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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JH295 Chemical Structure

JH295 Chemical Structure

CAS No. : 1311143-71-1

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5 mg USD 450 In-stock
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25 mg USD 1550 In-stock
50 mg USD 2350 In-stock
100 mg USD 3400 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1]. 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.

IC50 & Target

NEK2

770 nM (IC50)

Cellular Effect
Cell Line 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]
In Vitro

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.

Western Blot Analysis[1]

Cell Line: RPMI7951 cells
Concentration: 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 6.6 μM, 20 μM
Incubation Time: 45 minutes
Result: Inhibited WT Nek2 in cells with an IC50 of ~1.3 μM, whereas had little effect on the C22V mutant.
Molecular Weight

320.35

Formula

C18H16N4O2

CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

C#CC(NC1=CC2=C(NC(/C2=C\C3=C(C)N=C(CC)N3)=O)C=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1216 mL 15.6079 mL 31.2159 mL
5 mM 0.6243 mL 3.1216 mL 6.2432 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
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
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  • 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:
JH295
Cat. No.:
HY-116423
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