Catalog No.
Product Name
Application
Product Information
Citations
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PLK inhibitor
BI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations.- 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
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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).- Kishan Shamjibhai Italiya, .et al. , Ultrasound in Medicine & Biology, 2025, 51(7): 1124-1133
- Xiaofei Xin, .et al. , ACS Appl Mater Interfaces, 2019, 2019 PMID: 30933478
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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
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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/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
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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
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PLK inhibitor
NMS-1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. -
PLK inhibitor
SBE 13 HCl is a selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively). -
BTK inhibitor
LFM-A13 is a potent and selective inhibitor of Btk with IC50 of 17.2 uM; also inhibits PLK3 with IC50 of 7.2 uM. -
PLK4 inhibitor
Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM. -
PLK4 inhibitor
Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM. -
PLK1 inhibitor
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. -
multi-kinase inhibitor
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. -
PLK4 inhibitor
CFI-400945 is an orally active, potent and selective polo-like kinase 4(PLK4) inhibitor with Ki value of 0.26 nM. -
PLK4 inhibitor
CFI-400437 is a potent and selective inhibitor of polo-like kinase 4 (PLK4). -
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 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/BRD4 Inhibitor
PLK1/BRD4-IN-5 is a potent inhibitor targeting both PLK1 and BRD4, exhibiting IC50 values of 0.3 nM and 60.8 nM, respectively. This compound effectively induces cell cycle arrest in the S phase and promotes apoptosis in MV4-11 cells in a dose-dependent manner. PLK1/BRD4-IN-5 is a valuable tool for cancer research, facilitating studies on mechanisms of tumorigenesis and therapeutic responses. -
PLK4 Inhibitor
CZS-241 is a selective Polo-like Kinase 4 (PLK4) inhibitor, exhibiting an IC50 of 2.6 nM. In addition to its primary activity, CZS-241 also inhibits TRKA with an IC50 of 2.74 μM. This compound induces apoptosis and effectively arrests the cell cycle at the S/G2 phase. CZS-241 demonstrates potent antiproliferative effects against leukemia cell lines while maintaining safety profiles in normal cell lines, making it a valuable tool for cancer research. -
PLK1 Inhibitor
PLK1-IN-16 is a potent and selective inhibitor of polo-like kinase 1 (PLK1) with an IC50 value of 0.25 nM. This compound is primarily utilized in cancer research due to its ability to induce G2 phase cell cycle arrest and promote apoptosis, displaying significant antiproliferative activity against various tumor cell lines. Additionally, PLK1-IN-16 has been shown to exhibit stability under simulated gastric acid conditions and presents manageable CYP 450 inhibition. Its applications extend to the study of triple-negative breast cancer (TNBC), breast cancer, and leukemia. -
PLK4 Inhibitor
Ocifisertib hydrochloride is a potent inhibitor of Polo-like kinase 4 (PLK4) with a Ki value of 0.26 nM and an IC50 of 2.8 nM. This compound demonstrates significant biological activity by inhibiting the growth of various cancer cell lines, inducing cell cycle arrest at the G2/M phase, and promoting apoptosis. Research applications include evaluating its antitumor efficacy in preclinical models, making it a valuable reagent for studying mechanisms of cancer progression and potential therapeutic strategies. -
Dual PLK1/BET Inhibitor
WNY0824 is a dual inhibitor targeting Polo-like kinase 1 (PLK1) and the Bromodomain and Extra-Terminal (BET) protein family. It demonstrates potent inhibitory activity, with IC50 values of 22 nmol/L for PLK1 and varying efficacy against BRD2, BRD3, BRD4, and BRDT. WNY0824 induces cell cycle arrest and apoptosis by disrupting AR- and MYC-mediated transcriptional processes, making it valuable for research in cancer biology. Furthermore, it has shown effectiveness in inhibiting tumor growth in Enzalutamide-resistant castration-resistant prostate cancer (CRPC) xenograft models, highlighting its potential in overcoming treatment resistance. -
PLK Inhibitor
Poloxipan is a pan-specific inhibitor targeting polo-like kinases (PLKs), specifically interfering with the Polo-box domain at the C-terminus. It demonstrates IC50 values of 3.2 μM, 1.7 μM, and 3.0 μM against PLK-1, PLK-2, and PLK-3, respectively. Additionally, Poloxipan inhibits various phospho-tyrosine binding domains, including the forkhead-associated domain of CHK-2 and the WW domain of peptidyl-prolyl cis/trans isomerase (PIN1). This compound is valuable for applications in cancer research, particularly in studies involving PLK pathways and associated cellular processes. -
PLK1 PBD Inhibitor
MCC1019 is a selective inhibitor of the Polo-like kinase 1 (PLK1) phosphopeptide-binding domain (PBD), exhibiting an IC50 of 16.4 μmol/L. This compound effectively inactivates the AKT signaling pathway in cancer cells, leading to the induction of apoptosis, necroptosis, and autophagy. MCC1019 demonstrates significant anticancer activity against lung and prostate cancer, making it a valuable tool for cancer research and therapeutic studies. -
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. -
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. -
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. -
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.
