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

Centrinone  (Synonyms: LCR-263)

Cat. No.: HY-18682 Purity: 98.57%
COA Handling Instructions

Centrinone (LCR-263) 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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 201 In-stock
Solution
10 mM * 1 mL in DMSO USD 201 In-stock
Solid
1 mg USD 68 In-stock
5 mg USD 144 In-stock
10 mg USD 240 In-stock
50 mg USD 1080 In-stock
100 mg USD 2040 In-stock
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Customer Review

Based on 19 publication(s) in Google Scholar

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Description

Centrinone (LCR-263) 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 (LCR-263) 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 (LCR-263) 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 (LCR-263) reduces centriole number in multiciliated Xenopus epithelial cells, which indicates that Plk4 also controls centriole amplification in differentiated cells. Centrinone (LCR-263) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

633.65

Formula

C26H25F2N7O6S2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (48.92 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.95 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.95 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 98.57%

References
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 (LCR-263) 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
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Centrinone Related Classifications

Help & FAQs
  • 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:
Centrinone
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HY-18682
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