Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM.
IC50&Target
PLK4
0.59 nM (Ki)
PLK4 (G95L)
497.53 nM (Ki)
Aurora A
1239 nM (Ki)
Aurora B
5597.14 nM (Ki)
体外研究
Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM. Centrinone-B slightly binds to Aurora A and Aurora B, with Kis of 1239 nM and 5597.14 nM. Centrinone-B (LCR-323) 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. Centrinone-B (LCR-323) (0-200 nM) significantly decreases cell viability of PLK4-centriole conjunction melanoma cell lines except p53 mutant SK-MEL-28, and this effect is via inhibition of PLK4. Inhibition of PLK4 by Centrinone-B (LCR-323) also induces apoptosis in human melanoma cell lines.
分子式
C27H27F2N7O5S2
分子量
631.67
CAS号
1798871-31-4
运输条件
Room temperature in continental US; may vary elsewhere.