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Chemical Structure| 1798871-30-3 Chemical Structure| 1798871-30-3

Structure of Centrinone
CAS No.: 1798871-30-3

Chemical Structure| 1798871-30-3

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Centrinone is a selective and reversible inhibitor of polo-like kinase 4 (Plk4), a serine-threonine protein kinase that initiates centriole/centrosome assembly.

Synonyms: LCR-263

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Product Details of Centrinone

CAS No. :1798871-30-3
Formula : C26H25F2N7O6S2
M.W : 633.65
SMILES Code : CC1=CC(NC2=NC(SC3=CC=C(S(=O)(CC4=CC=CC([N+]([O-])=O)=C4F)=O)C=C3F)=NC(N5CCOCC5)=C2OC)=NN1
Synonyms :
LCR-263
MDL No. :MFCD28969654
InChI Key :HHJSKDRCUMVWKF-UHFFFAOYSA-N
Pubchem ID :91801159

Safety of Centrinone

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

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

In Vitro:

Cell Line
Concentration Treated Time Description References
NIH/3T3 mouse embryonic fibroblasts 100 nM depleted centrosomes Science. 2015 Jun 5;348(6239):1155-60
A375 cells 200 nM 4 days Induced centrosome overduplication Elife. 2022 Jun 27;11:e73944
RPE-1 cells 500 nM 4 days Resulted in cells containing either a single or no centrosome Elife. 2022 Jun 27;11:e73944
HCT116 cells 100 nM 4 days Observed the dynamic properties of NuMA in acentrosomal spindle poles, finding that NuMA is more static in acentrosomal spindle poles. EMBO J. 2020 Jan 15;39(2):e102378
HeLa cells 100 nM 3-5 days Induced the formation of acentrosomal spindles to study the mechanism of spindle bipolarity establishment in human somatic cells without centrosomes. EMBO J. 2020 Jan 15;39(2):e102378
HeLa cells 125 nM at least 4 days Depletion of centrosomes by inhibiting Plk4 activity to verify the effect of Centrinone on centrosome depletion Proc Natl Acad Sci U S A. 2016 Oct 25;113(43):E6590-E6599
hTERT-RPE1 immortalized retinal pigment epithelial cells (RPE1 cells) 150 nM 5 days To analyze the effect of centrosome removal in normal and cancer cells, centrinone treatment was found to block centriole duplication, leading to p53-dependent G1 arrest J Cell Biol. 2016 Jul 18;214(2):155-66
RPE-1 cells 200 nM 4 days Induced centrosome overduplication, resulting in approximately 50% of cells with supernumerary centrosomes Elife. 2022 Jun 27;11:e73944
8305c cells 0, 2, 4, 8, 16, 32 and 64 nM 72 h Centrinone decreased cell viability, induced cell apoptosis, arrested cell cycle at G2/M phase and inactivated Wnt/β-catenin signaling in a dose-dependent manner. Cancer Biol Ther. 2023 Dec 31;24(1):2223383
C643 cells 0, 2.5, 5, 10, 20, 40 and 80 nM 72 h Centrinone decreased cell viability, induced cell apoptosis, arrested cell cycle at G2/M phase and inactivated Wnt/β-catenin signaling in a dose-dependent manner. Cancer Biol Ther. 2023 Dec 31;24(1):2223383
HeLa cells 100 nM Centrinone 20 h Inhibition of Plk4 kinase activity induced irregular, non-spherical assemblies of GFP-Plk4 Nat Commun. 2019 Apr 18;10(1):1810
HeLa human cervical carcinoma cells 100 nM 7 days led to a progressive reduction in foci containing centriolar and pericentriolar material markers at each round of cell division, until most cells lacked centrioles and centrosomes Science. 2015 Jun 5;348(6239):1155-60
CHP134 neuroblastoma cells 150 nM 3 cell cycles To assess the effect of TRIM37 levels on sensitivity to PLK4 inhibition. CHP134 cells with high TRIM37 expression ceased proliferation following centrinone treatment, suggesting synthetic lethality with PLK4 inhibition. Nature. 2020 Sep;585(7825):440-446
RPE1 cells 150 nM 3 cell cycles To assess the effect of PLK4 inhibition on mitosis. Following centrinone treatment, chromosome segregation fails in ~10% of cells, leading to eventual growth arrest. Nature. 2020 Sep;585(7825):440-446

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.58mL

0.32mL

0.16mL

7.89mL

1.58mL

0.79mL

15.78mL

3.16mL

1.58mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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