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PLK inhibitors act on polo-like kinases (PLKs), serine/threonine kinases that coordinate mitosis and cytokinesis. The founding gene, polo, was described in Drosophila in 1991 as a protein kinase homolog required for mitosis. In PLK1, the most widely studied human member, a C-terminal polo-box domain (PBD) binds phosphorylated partner proteins and directs the kinase to its sites of action. BI 2536, reported in 2007, competes with adenosine triphosphate (ATP) and arrests cells in prometaphase. Volasertib, GSK461364 and TAK-960 are further ATP-competitive inhibitors used to study PLK1 in mitosis. Poloxin, described in 2008, works differently by blocking protein interactions that depend on the PBD.
Cyclapolin 9 is a selective ATP-competitive inhibitor of polo-like kinase 1 (PLK1) with an IC50 of 500 nM. This compound demonstrates potent inhibition specifically against PLK1, making it a valuable tool for studying cell cycle regulation and cancer biology. Its selectivity and efficacy support research applications focused on tumorigenesis and targeted cancer therapies.
Dihydrobaicalein is a selective PLK1 inhibitor, exhibiting an IC50 of 6.3 μM. This compound also demonstrates inhibitory activity against VRK2 and PLK2, making it a valuable tool in cancer research. Derived from the natural source Scutellaria scandens, dihydrobaicalein is utilized in studies exploring cell cycle regulation and mitotic processes. Its ability to modulate specific kinases positions it as a significant candidate for further investigation in therapeutic applications.
PLK1-IN-11 is a selective inhibitor of Polo-like kinase 1 (PLK1), exhibiting an IC50 of 1 μM. This compound demonstrates significant potential for modulating cell proliferation and mitotic progression. PLK1-IN-11 is suitable for investigation in various cancer models, including pancreatic, ovarian, breast, and non-small cell lung carcinoma, contributing to the understanding of cancer biology and the development of targeted therapies.
BTO-1 is a selective inhibitor of Polo-like kinase (Plk), a key regulator of the cell cycle. This compound is designed to interfere with Plk activity, impacting downstream phosphorylation and dephosphorylation processes. BTO-1 is utilized in research focused on cell cycle regulation, cancer biology, and the development of novel therapeutic strategies targeting Plk pathways.
PROTAC PLK1 Degrader-3 is a PLK1-targeted PROTAC that facilitates the degradation of the Polo-like kinase 1 (PLK1) protein through the N-deglycosylation pathway, exhibiting a dissociation constant (Kd) of 2.2 μM. This compound is primarily utilized in research related to non-small cell lung cancer, enabling investigations into targeted protein degradation mechanisms. While the compound shows limited cell penetration, higher concentrations may be necessary to achieve effective degradation outcomes, making it suitable for various biological studies in oncological contexts.
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DAP-81 is a potent inhibitor of Polo-like kinases (PLKs), a group of essential serine/threonine kinases involved in cell cycle regulation. This compound has been shown to dose-dependently increase the formation of monopolar spindles in treated cells, indicating its role in disrupting normal mitotic spindle assembly. High-resolution live-cell microscopy studies demonstrate that PLK activity is crucial for the integrity of bipolar mitotic spindles. By inhibiting PLK activity, DAP-81 destabilizes centromeric microtubules while enhancing the stability of other spindle microtubules, making it a valuable tool for researchers investigating cell division and potential anti-microtubule agents.
CAP-53194 is a selective inhibitor of Polo-like Kinase 1 (PLK1) with promising anticancer properties. It demonstrates significant selectivity, showing over 100-fold inhibition of PLK1 compared to PLK2-4 and other cell cycle-related kinases due to its ability to target unique features within the PLK1 binding site. CAP-53194 conforms to Lipinski's rule of five and meets various ADMET criteria, suggesting favorable pharmacokinetic characteristics. This compound represents a novel class of potential PLK1 inhibitors for further research and development in cancer therapeutics.
PLK1/PRC1-IN-1 is an inhibitor of the PLK1/PRC1 protein complex formation. This compound specifically targets the interaction between polo-like kinase 1 (PLK1) and protein-regulator of cytokinesis 1 (PRC1), disrupting their function. PLK1/PRC1-IN-1 is primarily utilized in research focused on non-small cell lung cancer (NSCLC) and provides insights into the mechanisms of cell division and tumor growth.
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CFI-400437 is an indolinone-derived, ATP-competitive inhibitor specifically targeting PLK4, exhibiting exceptional selectivity with an IC50 of 0.6 nM. This compound demonstrates potent inhibitory activity, making it a valuable tool for studying the role of PLK4 in cell cycle regulation and genomic stability. It is particularly useful in cancer research, where PLK4 dysregulation has been implicated in tumorigenesis.
PLK4-IN-3 is a selective inhibitor targeting Polo-like kinase 4 (PLK4), exhibiting an IC50 value of 0.65 μM. This compound plays a critical role in disrupting cell division by modulating the function of PLK4, which is essential for cytokinesis and centriole biogenesis. PLK4-IN-3 is valuable in cancer research, particularly in studies investigating the proliferation and survival of cancer cells with dysregulated PLK4 activity.
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PLK1-IN-5 is a selective inhibitor of Polo-like Kinase 1 (PLK1), with an IC50 of less than 500 nM. This compound demonstrates significant anticancer activity, making it a valuable tool for researchers studying cancer biology and therapeutic interventions. Its ability to effectively inhibit PLK1 offers potential applications in the development of novel cancer treatments.
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PLK1-IN-4 is a highly selective and potent inhibitor of Polo-like kinase 1 (PLK1), exhibiting an IC50 of less than 0.508 nM. It demonstrates significant antiproliferative effects across a range of cancer cell lines and induces mitotic arrest at the G2/M checkpoint, thereby promoting apoptotic pathways in cancer cells. This compound is valuable for investigations into hepatocellular carcinoma and other malignancies where PLK1 plays a critical role in cell cycle regulation.
PLK1-IN-2 is a potent inhibitor of the polo-like kinase 1 (PLK1), exhibiting an IC50 value of 0.384 μM. This compound disrupts PLK1 activity, which is crucial for regulating cell division and cancer cell proliferation. It is primarily utilized in cancer research to investigate the role of PLK1 in tumorigenesis and to assess its potential as a therapeutic target.
POI ligand-4 is a selective ligand for Polo-like kinase 1 (PLK1), serving as a crucial building block in the development of PROTACs. This compound facilitates targeted degradation of PLK1, exemplified in the synthesis of PROTAC PLK1 Degrader-3. It is instrumental in advancing research on cancer therapies and PLK1-related pathways.
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PLK1-IN-10 is a potent inhibitor of the polo-like kinase 1 (PLK1) polo-box domain. This compound disrupts the interaction between PLK1 and the cell division regulator protein PRC1, leading to a reduction in the expression of the CDK1-Cyclin B1 complex. Additionally, PLK1-IN-10 interacts with glutathione (GSH), increasing cellular oxidative stress and promoting apoptosis. Its applications include cancer research and studies on cell cycle regulation.
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TAK-960 monohydrochloride is a selective inhibitor of polo-like kinase 1 (PLK1), exhibiting an IC50 of 0.8 nM. It also demonstrates inhibitory effects on PLK2 and PLK3 with IC50 values of 16.9 nM and 50.2 nM, respectively. This compound effectively inhibits the proliferation of various cancer cell lines and shows significant antitumor activity in multiple tumor xenograft models, making it a valuable tool for cancer research applications.
ZK-Thiazolidinone is a potent ATP-competitive inhibitor of Polo-like kinase 1 (Plk1), exhibiting an IC50 of 19 nM. It effectively inhibits tumor cell proliferation, induces cell cycle arrest, and causes characteristic mitotic defects. The compound disrupts the recruitment of γ-tubulin and Aurora A kinase to centrosomes, leading to compromised bipolar spindle maintenance and sister chromatid cohesion. ZK-Thiazolidinone is valuable for applications in cancer research.
PLK1-IN-7 is a highly effective inhibitor of Polo-like kinase 1 (PLK1), demonstrating an IC50 of 0.66 nM. This compound exhibits significant antiproliferative and antitumor activities, making it a valuable tool for cancer research. Its ability to modulate PLK1 activity supports investigations into cell cycle regulation and potential therapeutic applications in oncology.
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IIP0943 is a potent and selective inhibitor of PLK1 (polo-like kinase 1), exhibiting an IC50 of 5.1 nM. This compound demonstrates significant antiproliferative activity against HCT116 cancer cells, with an IC50 of 0.22 µM. IIP0943 is a valuable tool for researchers investigating cancer therapeutics and the role of PLK1 in cell cycle regulation and tumor growth.
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Poloxin-2 is a specific inhibitor of Polo-like Kinase 1 (PLK1), effectively inducing mitotic arrest in HeLa cells with an EC50 of approximately 15 μM. It targets the Polo-box domain to disrupt protein-protein interactions, facilitating its application in cancer research. The hydrophobic tag (HT) conjugated form, Poloxin-2HT, exhibits enhanced potency by promoting selective degradation of the PLK1 protein, resulting in increased apoptosis and reduced cell viability. This highlights the potential of hydrophobic tags as a novel strategy for targeting disease-associated proteins.
PLK1-IN-9 is a potent inhibitor of polo-like kinase 1 (PLK1) that shows effective inhibition of modified PLK proteins, specifically 1010pT, cdc25c, and PBIP, with IC50 values of 1.6, 0.8, and 1.4 μM, respectively. This compound exhibits significant antiproliferative effects on various cancer cell lines, including HeLa, HL60, SNU387/499, and HepG2, where it induces cytotoxicity and apoptosis. In vivo studies demonstrate that PLK1-IN-9 effectively inhibits tumor growth in a HepG2 xenograft mouse model, highlighting its potential for cancer research applications.
CD 10899 is a potent Polo-like kinase 1 (PLK1) inhibitor, exhibiting an IC50 of 6 nM. As a hydroxylated metabolite of Volasertib, CD 10899 demonstrates significant pharmacological activity against PLK1, an important target in cancer research. This compound is valuable for studies exploring PLK1's role in cell cycle regulation and tumor progression, making it a useful tool for cancer-related investigations.
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