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

Centrinone-B 

Cat. No.: HY-18683 Purity: 98.58%
Handling Instructions

Centrinone-B is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM.

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

Centrinone-B Chemical Structure

Centrinone-B Chemical Structure

CAS No. : 1798871-31-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 200 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

Centrinone-B is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM.

IC50 & Target[1]

PLK4

0.59 nM (Ki)

PLK4 (G95L)

497.53 nM (Ki)

Aurora A

1239 nM (Ki)

Aurora B

5597.14 nM (Ki)

In Vitro

Centrinone-B is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM. Centrinone-B slightly binds to Aurora A and Aurora B, with Kis of 1239 nM and 5597.14 nM. Centrinone B exhibits >1000-fold selectivity for Plk4 over Aurora A/B in vitro and does not affect cellular Aurora A or B substrate phosphorylation at concentrations that deplete centrosomes[1]. Centrinone B (0-200 nM) significantly decreases cell viability of PLK4-centriole conjunction melanoma cell lines except p53 mutant SK-MEL-28, and this effect is via inhibition of PLK4. Inhibition of PLK4 by Centrinone B also induces apoptosis in human melanoma cell lines[2].

Solvent & Solubility
In Vitro: 

DMSO : 8.5 mg/mL (13.46 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5831 mL 7.9155 mL 15.8311 mL
5 mM 0.3166 mL 1.5831 mL 3.1662 mL
10 mM 0.1583 mL 0.7916 mL 1.5831 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

All kinase assays are performed in white 384-well plates. Plk4 assays use equal volumes of: (1) purified 6xHis-tagged human Plk4 kinase domain (aa 2-275) (expressed in E. coli and purified via Ni-NTA affinity chromatography) in 20 mM Tris pH 7.5, 100 mM NaCl, 10% glycerol, 1 mM DTT; (2) 2X reaction buffer consisting 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 (amino acid sequence: TPSDSLIYDDGLS). The Plk4 concentration in the final reaction is 2.5-10 nM with a final pH of 8.0. Inhibitors arrayed 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 Infinite M1000 plate reader. Data are fit using Prism and Kis are calculated from IC50 data[1].

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

Cell Assay
[2]

The effect of centrinone B on melanoma cell line and normal melanocyte viability is determined using the CytoTox-Glo assay. Briefly, cells are counted and plated in a 96-well plate and next day, treated with centrinone B for 48 hours, followed by incubation for 15 min with AAF-Glo substrate (alanyl-alanylphenylalanyl-aminoluciferin), which determines a distinct intracellular protease activity related with cytotoxicity (dead-cell protease) via a luminescent signal. Cell viability is determined by subtracting the luminescent signals of dead cells (due to centrinone B) from total dead cells (after addition of digitonin to lyse remaining viable cells). Data are represented as relative light units (RLU) for viable cells[2].

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

References
Molecular Weight

631.67

Formula

C₂₇H₂₇F₂N₇O₅S₂

CAS No.

1798871-31-4

SMILES

FC(C([N+]([O-])=O)=CC=C1)=C1CS(C2=CC(F)=C(SC3=NC(NC4=NNC(C)=C4)=C(OC)C(N5CCCCC5)=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

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Product Name:
Centrinone-B
Cat. No.:
HY-18683
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Centrinone-B

Cat. No.: HY-18683