Catalog No.
Product Name
Application
Product Information
Citations
-
PLK inhibitor
BI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations.- Giuseppe Madaro, .et al. , Neurogastroenterol Motil, 2026, Feb;38(2):e70259 PMID: 41639608
- Kyohei Matsuhashi, .et al. , Nat Commun, 2025, Sep 8;16:7799 PMID: 40921755
- Masae Ikura, .et al. , J Biochem, 2025, Jul 31;178(2):97-107 PMID: 40441713
- Ryuzaburo Yuki, .et al. , Eur J Pharmacol, 2024, Jan 15:963:176229 PMID: 38072041
- Nuria Gallisa-Sune, .et al. , Nat Commun, 2023, Apr 27;14(1):2434 PMID: 37105961
- Kei K Ito, .et al. , J Cell Biol, 2021, Mar 1;220(3):e202005153 PMID: 33492359
- Ryuzaburo Yuki, .et al. , J Cell Mol Med, 2021, Feb;25(3):1677-1687 PMID: 33465289
- Yamagishi A, .et al. , Int J Mol Sci, 2020, Feb 5;21(3) PMID: 32033461
- Bucko PJ, .et al. , Elife, 2019, Dec 24;8. pii: e52220 PMID: 31872801
- Watanabe K, .et al. , Nat Commun, 2019, Feb 25;10(1):931 PMID: 30804344
- Valérian Pasche, .et al. , Parasit Vectors, 2018, 11: 298 PMID: 29764454
- Takeshi Wakida, .et al. , eLife, 2017, 6: e29953 PMID: 29254517
- Majid Momeny, .et al. , Sci Rep, 2017, 7: 4204 PMID: 28646172
- Ifuji A, .et al. , Exp Cell Res, 2017, Nov 15;360(2):347-357 PMID: 28942021
-
PLK Inhibitor
BI6727 is a highly potent and selective polo-like kinase (PLK) 1 inhibitor (enzyme IC50 = 0.87 nM, EC50 = 11-37 nM on a panel of cancer cell lines).- Jianguo Huang, .et al. , JCI Insight, 2026, Jun 30:e192686 PMID: 42378032
- Kishan Shamjibhai Italiya, .et al. , Ultrasound in Medicine & Biology, 2025, 51(7): 1124-1133 PMID: 40234152
- Xiaofei Xin, .et al. , ACS Appl Mater Interfaces, 2019, 2019 PMID: 30933478
-
PLK1/PLK3 inhibitor
GW843682X is a selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC50 values are 2.2 and 9.1 nM respectively).- Kanada F, .et al. , Sci Rep, 2019, Dec 27;9(1):20085 PMID: 31882756
-
PLK1 inhibitor
MLN0905 is a potent, selective small-molecule PLK1 inhibitor. MLN0905 inhibits cell proliferation in a broad range of human tumor cells including DLBCL cell lines.- Reyhane Piri, .et al. , Invest New Drugs, 2025, Apr;43(2):348-356 PMID: 40278989
-
PLK Inhibitor
HMN-214 inhibits polo-like and cyclin-dependent kinase activity, has potent antimicrotubular effects and results in profound apoptosis and antitumor activity in a broad spectrum of human xenografts.- Yao-Yu Hsieh, .et al. , Mol Oncol, 2023, Oct 16 PMID: 37842807
-
PLK Inhibitor
ON-01910 is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. -
PLK1 Inhibtor
PLK1-IN-13 is a selective inhibitor of polo-like kinase 1 (PLK1) with an IC50 of 0.27 nM, exhibiting oral bioavailability. It also demonstrates inhibitory activity against PLK2 and PLK3, with IC50 values of 12.72 nM and 4.12 nM, respectively. PLK1-IN-13 effectively induces G2 phase cell cycle arrest, promotes apoptosis, and down-regulates the c-MYC oncogene, which is associated with tumor proliferation. This compound is particularly relevant for research on acute myeloid leukemia (AML) and other cancer models. -
PLK1 Inhibitor
PLK1-IN-15 is a potent inhibitor of Polo-like Kinase 1 (PLK1) with an IC50 of 38.5 nM. It demonstrates significant antiproliferative effects in various cancer cell lines, including HepG2, Huh7, H1299, and A549, with IC50 values of 2.03, 2.08, 4.79, and 17.11 μM, respectively. PLK1-IN-15 is known to induce cell cycle arrest at the G2/M phase and trigger apoptosis, underscoring its potential as an effective agent in cancer research and therapeutic development. -
PLK2 Inhibitor
ON1231320 is a selective inhibitor of polo-like kinase 2 (PLK2), exhibiting an IC50 of 0.31 μM. This compound disrupts tumor cell cycle progression specifically at the G2/M phase during mitosis, leading to apoptotic cell death. The arylsulfonyl pyrido-pyrimidinone structure contributes to its significant antitumor activity, making ON1231320 a valuable tool for research in cancer biology and therapeutic development. -
PLK1 Inhibitor
Volasertib trihydrochloride is a potent, ATP-competitive inhibitor of Polo-like kinase 1 (PLK1) with an IC50 of 0.87 nM. This compound also exhibits inhibitory activity against PLK2 and PLK3 with IC50s of 5 nM and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis in cancer cells, demonstrating significant antitumor efficacy across various cancer models. It is a valuable tool for research focused on cell division and the development of cancer therapeutics. -
PLK1/BRD4 Inhibitor
PLK1/BRD4-IN-3 is a selective dual inhibitor targeting bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). This compound effectively inhibits BRD4-BD1, PLK1, and BRDT-BD1, exhibiting IC50 values of 0.059 µM, 0.127 µM, and 0.245 µM, respectively. PLK1/BRD4-IN-3 can be employed in research applications focused on cancer biology, particularly in studies investigating cell proliferation and transcriptional regulation. -
PLK1/BRD4 Inhibitor
PLK1/BRD4-IN-2 is a dual inhibitor targeting both Polo-like kinase 1 (PLK1) and the bromodomain of BRD4, with an IC50 of 40 nM and 28 nM, respectively. This compound is valuable for research into cancer therapeutics and epigenetic regulation, demonstrating potential in studies focused on cell proliferation and transcriptional control. Its ability to simultaneously inhibit these key oncogenic pathways positions PLK1/BRD4-IN-2 as a crucial tool for advancing cancer research and drug discovery initiatives. -
PLK1/p38γ Inhibitor
PLK1/p38γ-IN-1 is a multitarget inhibitor that selectively targets PLK1 and p38γ kinases. This compound has demonstrated the ability to inhibit cell proliferation in human hepatocellular carcinoma and hepatoblastoma cell lines in vitro. PLK1/p38γ-IN-1 is valuable for research focused on cancer biology and the modulation of cell cycle pathways. -
PLK2 Inhibitor
8012-3246 is a selective inhibitor of Polo-like kinase 2 (PLK2) with an IC50 of 774.5 nM. This compound effectively suppresses the phosphorylation of GSK3β, demonstrating its potential role in cellular signaling modulation. Additionally, 8012-3246 exhibits significant anticancer activity, particularly against colorectal cancer, making it a valuable tool for cancer research applications focusing on PLK2-related pathways. -
p53-Y220C/PLK1 Modulator
p53-Y220C/PLK1 modulator-1 is a novel dual modulator targeting the p53-Y220C mutation and Polo-like kinase 1 (PLK1). This compound exhibits significant biological activity in cancer research, providing a potential therapeutic avenue for tumors harboring the p53-Y220C alteration. Its application in cellular and molecular studies can facilitate the exploration of p53-mediated pathways and PLK1 functionality in oncogenesis. -
PLK-1/Tubulin Inhibitor
3,4,3'-Tri-O-methylflavellagic acid is a flavonoid compound that functions as an inhibitor of polo-like kinase-1 (PLK-1) and αβ-tubulin at the colchicine binding site. This compound disrupts microtubule assembly dynamics and modulates kinase activity, making it valuable for research into cancer cell proliferation and anti-nociceptive properties. Its unique biological activities make it a significant reagent for studies focused on cancer therapies and pain management. -
TTK/PLK1 Inhibitor
TTK/PLK1-IN-1 is a potent inhibitor of threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1), demonstrating IC50 values of 7 nM and 72 nM, respectively. This compound plays a crucial role in regulating the spindle assembly checkpoint (SAC), making it relevant for cancer research. It exhibits promising antitumor activity against triple-negative breast cancer (TNBC), contributing to its potential applications in oncology studies. -
PLK1 Inhibitor
GSK461364 analogue 1 is a thiophene-based inhibitor targeting Polo-like kinase 1 (PLK1), exhibiting an IC50 value of 2 nM, along with inhibitory activity against PLK3 (IC50: 630 nM) and Nek2 kinase (IC50: 21 nM). With a solubility of ≥190 μM in pH 7.4 PBS and a human plasma protein binding rate of 91.5%, this compound is suitable for in vitro studies. GSK461364 analogue 1 is particularly relevant for research into malignancies such as colon, lung, breast, and ovarian cancers. -
PLK2 Inhibitor
Y207–5465 is a potent and highly selective inhibitor of Polo-like kinase 2 (PLK2), exhibiting an IC50 value of 584.3 nM. This compound demonstrates limited anti-cancer activity in human colorectal cancer cell lines HT-29 and HCT-116. It is suitable for use in cancer research, providing insights into the role of PLK2 in tumorigenesis and therapeutic resistance. -
PLK4 Inhibitor
Ocifisertib fumarate is a potent and selective inhibitor of Polo-like kinase 4 (PLK4), exhibiting a Ki value of 0.26 nM and an IC50 of 2.8 nM. This compound demonstrates significant biological activity in the modulation of cell cycle progression and centrosome duplication. Ocifisertib fumarate is primarily utilized in research focused on cancer biology, particularly in studies assessing the role of PLK4 in tumorigenesis and potential therapeutic interventions targeting this kinase. -
PLK1 Inhibitor
Plogosertib is a selective and potent ATP-competitive inhibitor of the polo-like kinase 1 (PLK1) with an IC50 of 3 nM. This compound exhibits significant anti-proliferative activity, making it a valuable agent in cancer research. Plogosertib is applicable in studies involving various malignancies, including esophageal, gastric, leukemia, non-small cell lung cancer, ovarian, and squamous cell cancers. -
PLK4 Inhibitor
RP-1664 is a selective and orally active inhibitor of Polo-like kinase 4 (PLK4) with an IC50 of 3 nM. This compound exhibits remarkable selectivity toward PLK4 compared to related kinases such as AURKA, AURKB, and PLK1. RP-1664 disrupts centriole biogenesis in cancer cells, resulting in the accumulation of PLK4 and p21 proteins. Its anti-tumor activity has been demonstrated in models of breast cancer and neuroblastoma, particularly in TRIM37-high-expressing cellular contexts. -
PLK4 Inhibitor
PLK4-IN-4 is a potent inhibitor of polo-like kinase 4 (PLK4), demonstrating an IC50 value of 7.9 nM. This compound effectively disrupts PLK4 activity, a critical regulator of centriole duplication, making it a valuable tool for cancer research. PLK4-IN-4 is suitable for studies investigating the role of PLK4 in tumorigenesis and may aid in the development of targeted cancer therapies. -
PROTAC PLK4 Degrader
SP27 is a PROTAC that selectively degrades Polo-like kinase 4 (PLK4), exhibiting a DC50 of 19.5 nM. This compound is valuable for investigating the role of PLK4 in cellular processes and is particularly relevant in breast cancer research, enabling studies on potential therapeutic applications and mechanisms of action related to oncogenesis. -
PLK4 Inhibitor
PLK4-IN-1 is a selective inhibitor of PLK4, exhibiting an IC50 of less than or equal to 0.1 μM. This compound plays a critical role in cell cycle regulation through the inhibition of polo-like kinase 4 activity. Its application is significant in research focusing on cell proliferation, cancer therapeutics, and understanding mitotic processes. -
PLK1 Inhibitor
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. -
PLK1 Inhibitor
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 Inhibitor
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. -
Plk Inhibitor
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. -
PLK1 PROTAC Degrader
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. -
Polo-like Kinase (PLK) Inhibitor
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. -
Polo-like Kinase (PLK)
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 Inhibitor
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. -
PLK4 Inhibitor
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 Inhibitor
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. -
PLK1 Inhibitor
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. -
PLK1 Inhibitor
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. -
PLK Inhibitor
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. -
PLK1 Ligand
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. -
PLK1 Inhibitor
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. -
PLK1 Inhibitor
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. -
Plk1 Inhibitor
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 Inhibitor
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. -
PLK1 Inhibitor
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. -
Polo-like Kinase (PLK) Inhibitor
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. -
PLK Inhibitor
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. -
PLK1 Inhibitor
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. -
PLK inhibitor
NMS-1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity.
