Home Cell Cycle PLK inhibitor Centrinone (LCR-263) For research use only.

Centrinone (LCR-263)

Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM.

Centrinone (LCR-263) Chemical Structure

Centrinone (LCR-263) Chemical Structure

CAS: 1798871-30-3

Purity & Quality Control

Batch: Purity: 99.17%
99.17

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Biological Activity

Description Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM.
Targets
PLK4 [1]
(Cell-free assay)
0.16 nM(Ki)
In vitro
In vitro

Centrinone (LCR-263) prevents centriole assembly by inhibiting Plk4Centrinone treatment causes centrosome depletion in human and other vertebrate cells.<sup><a class="sref" href="#s_ref">[1]</a></sup>
Kinase Assay
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. 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.
Cell Research Cell lines HeLa cells, NIH/3T3 cells
Concentrations 125 nM
Incubation Time 2 weeks
Method

For the first two days after centrinone addition, when cells retained 2 or 1 centrosomes, the proliferation of HeLa and NIH/3T3 cells was identical to controls; this was followed by a decrease in proliferation rate coincident with the appearance of centrosome-less cells. Long-term treated cells continued to proliferate at the slower rate, and returned to the control rate after wash-out-mediated centrosome recovery.

Chemical Information & Solubility

Molecular Weight 633.65 Formula

C26H25F2N7O6S2
CAS No. 1798871-30-3 SDF --
Smiles COC1=C(N=C(SC2=CC=C(C=C2F)[S](=O)(=O)CC3=CC=CC(=C3F)[N+]([O-])=O)N=C1NC4=N[NH]C(=C4)C)N5CCOCC5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (157.81 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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