Centrinone-B (LCR-323) (Synonyms: LCR-323) |
رقم الكتالوجGC32751 |
Centrinone-B (LCR-323) (LCR-323) هو مثبط PLK4 قوي وانتقائي للغاية ، مع Ki 0.59 نانومتر.
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Cas No.: 1798871-31-4
Sample solution is provided at 25 µL, 10mM.
Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM.
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[1]. 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[2].
[1]. 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. [2]. 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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