Structure
Centrinone-B, Inhibitor
Centrinone-B
Purity
98.00%
Synonyms
Centrinone-B; LCR-323; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 25mg/mL (39.58mM) Need ultrasonic
H2O: <0.1mg/mL (insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
H2O: <0.1mg/mL (insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C27H27F2N7O5S2
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
CAS Number
1798871-31-4
Target & IC50
PLK4: ic50 0.59nM (ki)
PLK4 G95L: ic50 497.53nM (ki)
Aurora A: ic50 1239nM (ki)
Aurora B: ic50 5597.14nM (ki)
PLK4 G95L: ic50 497.53nM (ki)
Aurora A: ic50 1239nM (ki)
Aurora B: ic50 5597.14nM (ki)
In Vitro
Centrinone-B (0-200nM) significantly decreases cell viability of PLK4-centriole conjunction melanoma cell lines except for p53 mutant SK-MEL-28, and this effect is via inhibition of PLK4. Centrinone-B slightly binds to Aurora A and Aurora B (Kis: 1239nM and 5597.14nM). 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]. Inhibition of PLK4 by Centrinone-B also induces apoptosis in human melanoma cell lines [2].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for Centrinone-B, inhibitor
Centrinone-B (LCR-323) is a potent and highly selective inhibitor of PLK4 (Ki: 0.59nM).
Product Categories/Family for Centrinone-B, inhibitor
References
Wong YL, et al. Cell biology. Reversible centriole depletion with an inhibitor of Polo-like kinase Science. 2015 Jun 5;348(6239):1155-60.
Wong YL, et al. Cell biology. Reversible centriole depletion with an inhibitor of Polo-like kinase 4. Science. 2015 Jun 5;348(6239):1155-60.
Denu RA, et al. Centriole Overduplication is the Predominant Mechanism Leading to Centrosome Amplification in Melanoma. Mol Cancer Res. 2018 Jan 12.
Denu RA, et al. Centriole Overduplication is the Predominant Mechanism Leading to Centrosome Amplification in Melanoma. Mol Cancer Res. 2018 Jan 12.
Wong YL, et al. Cell biology. Reversible centriole depletion with an inhibitor of Polo-like kinase 4. Science. 2015 Jun 5;348(6239):1155-60.
Denu RA, et al. Centriole Overduplication is the Predominant Mechanism Leading to Centrosome Amplification in Melanoma. Mol Cancer Res. 2018 Jan 12.
Denu RA, et al. Centriole Overduplication is the Predominant Mechanism Leading to Centrosome Amplification in Melanoma. Mol Cancer Res. 2018 Jan 12.
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Product Notes
The Centrinone-B (Catalog #AAA5754697) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Centrinone-B, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
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Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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