Centrinone (LCR-263)

Catalog No.S7837 Batch:S783702

Technical Data

Formula	C₂₆H₂₅F₂N₇O₆S₂
Molecular Weight	633.65	CAS No.	1798871-30-3
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (157.81 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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>

Protocol (from reference)

Kinase Assay:^{<sup><a class="sref"href="#s_ref">[2]</a></sup>}	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 Assay:^{^[1]}	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.

Kinase Assay:^{<sup><a class="sref"href="#s_ref">[2]</a></sup>}

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 Assay:^{^[1]}

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.

References

[1] Yao Liang Wong, et al. Science. 2015 Jun 5;348(6239):1155-60.

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SHIPPING AND STORAGE
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