A thymoquinone derivative, non-ATP competitive Polo-like Kinase 1 (Plk1) inhibitor specifically targeting the polo-box domain (PBD) of Plk1 (IC50)=4.8uM. Reduces both chromosome and kinetochoral localization of Plk1, induces chromosome congression defects , mitotic arrest in prometaphase, and apoptosis in HeLa cells at 25uM. Exhibits anti-proliferative effects in a range of cancer cell lines, and in a mouse Xenograft model involving HeLa and MDA-MB-231 cells at 40mg/kg.
Formula:C₁₈H₁₉NO₃
Molecular Weight:297.4
Solubility:DMSO (25mg/ml, clear, yellow solution)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
