Centrinone

SKU: orb1218608

Description

Centrinone (LCR-263) is a reversible inhibitor of polo-like kinase 4 (PLK4; Ki:0.16 nM). (In Vitro):Centrinone (LCR-263) exhibits more than 1000-fold selectivity for Plk4 over Aurora A/B and does not affect cellular Aurora A or B substrate phosphorylation at concentrations that deplete centrosomes. 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. Treatment with Centrinone (LCR-263) reduces centriole number in multiciliated Xenopus epithelial cells, which indicates that Plk4 also controls centriole amplification in differentiated cells. Centrinone (LCR-263) treatment causes centrosome depletion in human and other vertebrate cells. 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.

Key Properties

• CAS Number: 1798871-30-3
• MW: 633.65
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₅F₂N₇O₆S₂
• SMILES: CC1=CC(NC2=NC(SC3=CC=C(S(=O)(CC4=CC=CC([N+]([O-])=O)=C4F)=O)C=C3F)=NC(N5CCOCC5)=C2OC)=NN1
• Target: Aurora Kinase
• Solubility: DMSO:31 mg/mL (48.92 mM)

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LCR-263

Quick Database Links

Gene Symbol

Aurora Kinase