1. Cell Cycle/DNA Damage
  2. Polo-like Kinase (PLK)

Centrinone 

Cat. No.: HY-18682 Purity: 98.02%
Handling Instructions

Centrinone is a selective and reversible inhibitor of polo-like kinase 4 (PlK4) with a Ki of 0.16 nM.

For research use only. We do not sell to patients.

Centrinone Chemical Structure

Centrinone Chemical Structure

CAS No. : 1798871-30-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 201 In-stock
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Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1080 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 2040 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Centrinone:

Customer Validation

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Centrinone is a selective and reversible inhibitor of polo-like kinase 4 (PlK4) with a Ki of 0.16 nM.

IC50 & Target[1]

PLK4

0.16 nM (Ki)

PLK4 (G95L)

68.57 nM (Ki)

Aurora A

171 nM (Ki)

Aurora B

436.76 nM (Ki)

In Vitro

Centrinone exhibits more than 1000-fold selectivity for Plk4 over Aurora A/B and does not affect cellular Aurora A or B substrate phosphorylation at concentrations that deplete centrosomes. Centrinone treatment of HeLa human cervical carcinoma cells leads to a progressive reduction in foci containing centriolar and pericentriolar material markers at each round of cell division, until most cells lack centrioles and centrosomes. Treatment with centrinone reduces centriole number in multiciliated Xenopus epithelial cells, which indicates that Plk4 also controls centriole amplification in differentiated cells. Centrinone treatment causes centrosome depletion in human and other vertebrate cells. Centrosome loss irreversibly arrests normal cells in a senescence-like G1 state by a p53-dependent mechanism that is independent of DNA damage, stress, Hippo signaling, extends mitotic duration, or segregation errors[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.5782 mL 7.8908 mL 15.7816 mL
5 mM 0.3156 mL 1.5782 mL 3.1563 mL
10 mM 0.1578 mL 0.7891 mL 1.5782 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

Purified 6xHis-tagged human Plk4 kinase domain is in 20 mM Tris pH 7.5, 100 mM NaCl, 10% glycerol, 1 mM DTT. 2X reaction buffer consists of 50 mM HEPES pH 8.5, 20 mM MgCl2, 1 mM DTT, 0.2 mg/mL BSA, 16 μM ATP, and 200 μM A-A11 substrate. The Plk4 concentration in the final reaction is 2.5-10 nM with a final pH of 8.0. Inhibitors (Centrinone) array in dose response are added from DMSO stocks. Reactions are allowed to proceed for 4-16 hours at 25°C. Detection is performed using ADP-Glo reagent. Luminescence is measured on an plate reader[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

For each condition, cells are seeded in triplicate into 6-well plates at 50,000 cells/well. 125 nM centrinone is added to HeLa cells or 300 nM is added to NIH/3T3 cells. At 24-hour intervals, 3 wells are harvested per condition. Cell counting is performed using a TC10 automated cell counter[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

633.65

Formula

C₂₆H₂₅F₂N₇O₆S₂

CAS No.

1798871-30-3

SMILES

FC(C([N+]([O-])=O)=CC=C1)=C1CS(C2=CC(F)=C(SC3=NC(NC4=NNC(C)=C4)=C(OC)C(N5CCOCC5)=N3)C=C2)(=O)=O

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: ≥ 31 mg/mL

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

Purity: 98.02%

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Product Name:
Centrinone
Cat. No.:
HY-18682
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