Centrinone

SKU: orb1308467

Description

Centrinone (LCR-263) is a potent and reversible small-molecule inhibitor of PLK4 with a Ki of 0.16 nM. It is widely used in biochemical and cellular studies to investigate centriole duplication and has been applied in both in vitro assays and in vivo models to explore its effects on cell cycle progression and genome stability.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 1798871-30-3
• MW: 633.65
• Purity: 98.58% (May vary between batches)
• Formula: C₂₆H₂₅F₂N₇O₆S₂
• SMILES: COc1c(Nc2cc(C)[nH]n2)nc(Sc2ccc(cc2F)S(=O)(=O)Cc2cccc(c2F)[N+]([O-])=O)nc1N1CCOCC1
• Target: PLK,Aurora Kinase
• Solubility: DMSO:31 mg/mL (48.92 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (7.89 mM)

Bioactivity

• Target IC50:
  PLK4:0.16 nM (ki)|PLK4 (G95L):68.57 nM (ki)|Aurora B:436.76 nM (ki)|Aurora A:171 nM (ki)
• In Vitro:
  Centrinone (LCR-263) treatment causes centrosome depletion in human and other vertebrate cells and it treatment reduces centriole number in multiciliated Xenopus epithelial cells, which indicates that Plk4 also controls centriole amplification in differentiated cells. Centrinone (LCR-263) treatment of HeLa human cervical carcinoma cells leads to a progressive reduction in foci containing centriolar and pericentriolar material markers at each round of cell division, until most cells lack centrioles and centrosomes. Centrosome loss irreversibly arrests normal cells in a senescence-like G1 state by a p53-dependent mechanism that is independent of DNA damage, stress, Hippo signaling, extends mitotic duration, or segregation errors.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Polo-like Kinase (PLK), PLK, PLK4 G95L, PLK4, Centrinone, Aurora Kinase, AuroraKinase, Aurora B, Aurora A, inhibit, LCR263, LCR-263, LCR 263, Inhibitor

Compound Identifiers

PubChem CID

91801159