Centrinone-B (LCR-323) is a potent and highly selective inhibitor of PLK4 (Ki: 0.59 nM).

Centrinone-B (0-200 nM) 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: 1239 nM and 5597.14 nM). 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].

1798871-31-4

C27H27F2N7O5S2

631.67

LCR-323

DMSO:25 mg/mL (39.58 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years