1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase

ZM-447439 

Cat. No.: HY-10128 Purity: 98.88%
Handling Instructions

ZM-447439 is an aurora kinase inhibitor with IC50s of 110 and 130 nM for aurora A and B, respectively.

For research use only. We do not sell to patients.
ZM-447439 Chemical Structure

ZM-447439 Chemical Structure

CAS No. : 331771-20-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 68 In-stock
5 mg USD 60 In-stock
10 mg USD 90 In-stock
50 mg USD 312 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ZM-447439 is an aurora kinase inhibitor with IC50s of 110 and 130 nM for aurora A and B, respectively.

IC50 & Target

IC50: 110 nM (Aurora A), 130 nM (Aurora B)[1]

In Vitro

Cells treated with ZM-447439 progress through interphase, enter mitosis normally, and assemble bipolar spindles. However, chromosome alignment, segregation, and cytokinesis all fail. ZM-447439 inhibits cell division and inhibit mitotic phosphorylation of histone H3. ZM-447439 prevents chromosome alignment and segregation. ZM-447439 compromises spindle checkpoint function. ZM-447439 inhibits kinetochore localization of BubR1, Mad2, and Cenp-E[1]. Inhibition of Aurora kinase by ZM-447439 reduces histone H3 phosphorylation at Ser10 in Hep2 carcinoma cells. Multipolar spindles are induced in these ZM-treated G2/M-arrested cells with accumulation of 4N/8N DNA, similar to cells with genetically suppressed Aurora-B. ZM-447439 treatment induces cell apoptosis. ZM-447439 inhibition of Aurora kinase is potently in association with decrease of Akt phosphorylation at Ser473 and its substrates GSK3α/β phosphorylation at Ser21 and Ser9[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.9471 mL 9.7354 mL 19.4708 mL
5 mM 0.3894 mL 1.9471 mL 3.8942 mL
10 mM 0.1947 mL 0.9735 mL 1.9471 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

1 ng purified recombinant enzyme is added to a reaction cocktail containing buffer, 10 μM peptide substrate, 10 μM for Aurora A or 5 μM ATP for Aurora B, and 0.2 μCi γ[33P]ATP, and is then incubated at room temperature for 60 min. Reactions are stopped by addition of 20% phosphoric acid, and the products are captured on P30 nitrocellulose filters and assayed for incorporation of 33P with a Betaplate counter. No enzyme and no compound control values are used to determine the concentration of ZM-447439, which gave 50% inhibition of enzyme activity[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

ZM-447439 is dissolved in DMSO and freshly diluted in media[1].

To determine cloning efficiency, MCF7 cells are plated in phenol red free DME plus 5% stripped serum, and are then treated with or without the anti-estrogen ICI 182780 at 1 μM for 48 h. ZM-447439 is then added at the indicated concentrations for 72 h. The cells are harvested, washed, and ∼400 cells plated in each well of a 6-well plate in complete media without ZM-447439. After 10 d, the colonies are fixed, stained with crystal violet, and counted. The cloning efficiency represents the number of colonies on ZM-447439-treated plates compared with DMSO-treated controls[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

513.59

Formula

C₂₉H₃₁N₅O₄

CAS No.

331771-20-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
ZM-447439
Cat. No.:
HY-10128
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