PLK1
PLK1 is a serine/threonine Polo-like kinase that orchestrates cell division through mitotic entry, spindle-pole functions, and cytokinesis[1]. Mechanistically, mammalian PLK1 controls centrosome maturation, spindle assembly, and microtubule attachment to kinetochores in early mitosis[2]. This mitotic role makes PLK1 relevant to cancer biology, because dysfunction may promote cancerous transformation and drive progression, and overexpression occurs in diverse human cancers with poor prognosis[3]. Compared with related isoforms, PLK1-PLK4 participate in cell-cycle processes, but reported functional emphasis differs: PLK2 and PLK4 regulate centriole duplication, PLK3 regulates DNA replication, and PLK1 regulates centrosome separation and maturation[4]. For experimental applications, PLK1 inhibition provides a direct way to perturb mitosis, because BI 2536 inhibits mammalian PLK1 at low nanomolar concentrations, induces mitotic arrest and apoptosis in human cancer cell lines, and inhibits human tumor xenograft growth in nude mice[5].
References:
- [1]. Barr FA, et al. Polo-like kinases and the orchestration of cell division. Nat Rev Mol Cell Biol. 2004 Jun;5(6):429-40. [Content Brief]
- [2]. Santamaria A, et al. The Plk1-dependent phosphoproteome of the early mitotic spindle. Mol Cell Proteomics. 2011 Jan;10(1):M110.004457. [Content Brief]
- [3]. Liu Z, et al. PLK1, A Potential Target for Cancer Therapy. Transl Oncol. 2017 Feb;10(1):22-32. [Content Brief]
- [4]. de Cárcer G, et al. From Plk1 to Plk5: functional evolution of polo-like kinases. Cell Cycle. 2011 Jul 15;10(14):2255-62. [Content Brief]
- [5]. Steegmaier M, et al. BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo. Curr Biol. 2007 Feb 20;17(4):316-22. [Content Brief]
-
PLK1 Related Products (63)
Related Products (63)
-
Antibodies (3)
-
MCC1019
0 ImagesCat. No.: HY-W162436CAS No.: 29115-34-2MCC1019 is a selective PLK1 PBD inhibitor with an IC50 of 16.4 μmol/L. MCC1019 inactivates the AKT signaling pathway in cancer cells, and induces Apoptosis, Necroptosis and Autophagy. MCC1019 exhibits anticancer activity against lung cancer and prostate cancer.
-
ZNL-02-096
0 ImagesCat. No.: HY-208742CAS No.: 2414418-56-5ZNL-02-096 is a selective Wee1 PROTAC degrader. ZNL-02-096 binds to CRBN and Wee1 to form a ternary complex, inducing CRBN- and proteasome-dependent ubiquitination and proteasomal degradation of Wee1. ZNL-02-096 inhibits recombinant PLK1 with an IC50 of 102 nM, but does not induce its degradation in cells. ZNL-02-096 induces G2/M phase arrest, Apoptosis, transient integrated stress response, upregulation of ATF4, and phosphorylation of GCN2. ZNL-02-096 reduces Tyr15 phosphorylation of CDK1. ZNL-02-096 can be used in research related to ovarian cancer, acute lymphoblastic leukemia, triple-negative breast cancer, multiple myeloma, and pancreatic ductal adenocarcinoma.
-
WNY0824
0 ImagesCat. No.: HY-143471CAS No.: 2412707-81-2Synonyms: PLK1/BRD4-IN-1WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models.
-
Allopole-A
0 ImagesCat. No.: HY-188141CAS No.: 3057557-03-3Allopole-A is a Plk1 inhibitor with an IC50 of 1.4-2.5 μM against human Plk1 PBD1. Allopole-A binds to the allosteric W-F pocket in Plk1 PBD1, displacing the L2 loop, thereby disrupting water-mediated phospho-ligand binding interactions and promoting inhibitory interactions between the kinase domain and PBD to suppress Plk1 kinase activity. Allopole-A can be used in studies of human cancers with plk1 overexpression.
-
PLK1-IN-14
0 ImagesCat. No.: HY-173233PLK1-IN-14 (Compound Hit-4) is a selective PLK1 inhibitor. It has an IC50 of 22.61 pM against PLK1 and an IC50 of 0.09 nM for inhibiting the proliferation of DU - 145 prostate cancer cells. PLK1-IN-14 can be used in the research of prostate cancer.
-
GSK461364 analogue 1
0 ImagesCat. No.: HY-111090CAS No.: 929095-23-8GSK461364 analogue 1 is a thiophene-based PLK1 inhibitor with a PLK1 IC50 of 2 nM and a PLK3 IC50 of 630 nM. GSK461364 analogue 1 also acts as an inhibitor of Nek2 kinase (IC50: 21 nM). GSK461364 analogue 1 has a solubility of ≥190 μM in pH 7.4 PBS and a human plasma protein binding rate of 91.5%. GSK461364 analogue 1 can be used in studies related to colon cancer, lung cancer, breast cancer and ovarian cancer.
-
YLT-11
0 ImagesCat. No.: HY-115589CAS No.: 3040940-49-3
-
PLK1-IN-5
0 ImagesCat. No.: HY-148974CAS No.: 1001343-34-5PLK1-IN-5 is a potent PLK1 inhibitor with an IC50 of < 500 nM. PLK1-IN-5 shows anticancer effects (WO2008113711A1; compound I-4).
-
PLK1-IN-12
0 ImagesCat. No.: HY-172364PLK1-IN-12 is a highly selective and orally active PLK1 inhibitor with an IC50 of 20 nM. PLK1-IN-12 shows more selective for PLK1 than PLK2 (IC50: >10000 nM) and PLK3 (IC50: 3953 nM). PLK1-IN-12 exhibits anticancer potency across a broad spectrum of cell lines. PLK1-IN-12 can be used in anti-leukemia research.
-
Anticancer agent 306
0 ImagesCat. No.: HY-181769CAS No.: 3043892-01-6Anticancer agent 306 is a spiro tetramic acid derivative and a inhibitor of MMP1, MMP7 and PLK1. Anticancer agent 306 exerts antiproliferative activity against H1299, RKO and MCF-7 cells with IC50 values of 19.25 μM, 3.29 μM and 102.36 μM, respectively. Anticancer agent 306 can up-regulate p21 protein and down-regulate CCND1 and CCNB1 proteins to induce cell cycle arrest, regulate the expression of Bcl-2 and Bax to induce cell apoptosis. Anticancer agent 306 can down-regulate MMP1 and MMP7 proteins to inhibit tumor invasion and metastasis. Anticancer agent 306 can be used for the research of lung cancer, colorectal cancer, breast cancer.
-
3,4,3'-Tri-O-methylflavellagic acid
0 ImagesCat. No.: HY-N13795CAS No.: 13756-49-53,4,3'-Tri-O-methylflavellagic acid is a flavonoid inhibitor that targets αβ-tubulin (colchicine binding site) and polo-like kinase-1 (PLK-1), and can be isolated from the roots of Anogeissus leiocarpus. 3,4,3'-Tri-O-methylflavellagic acid interferes with microtubule assembly dynamics and kinase activity, exhibiting anti-cancer cell proliferation and potent anti-nociceptive effects.
-
PLK1-IN-10
0 ImagesCat. No.: HY-161521CAS No.: 2991469-21-5PLK1-IN-10 (Compound 4Bb) is an orally active PLK1 PBD (polo-box domain) inhibitor. PLK1-IN-10 blocks the interaction of PLK1 with the cell division regulator protein 1 (PRC1) and decreases the protein expression of the CDK1-Cyclin B1 complex. PLK1-IN-10 reacts with glutathione (GSH) to increase cellular oxidative stress, ultimately leading to cell death.
-
PLK2-IN-1
0 ImagesCat. No.: HY-189637PLK2-IN-1 is a selective PLK2 inhibitor (IC50 0.78 μM). PLK2-IN-1 induces Apoptosis and cell cycle arrest, reduces AKT and mTOR phosphorylation, and decreases Cyclin E expression as well as downregulates the CDK2/Rb/E2F1 axis. PLK2-IN-1 inhibits tumor growth in colorectal cancer xenograft models. PLK2-IN-1 can be used for research on colorectal cancer.
-
(S)-BI 2536
0 ImagesCat. No.: HY-50698ACAS No.: 1241725-90-5(S)-BI 2536 is the enantiomer of BI 2536 (HY-50698). (S)-BI 2536 acts as an inhibitor of the BRD4 bromodomain and PLK1 kinase, with a Ki value of 54 nM against BRD4 and a Ki value of 0.42 nM against PLK1 kinase. (S)-BI 2536 exhibits anticancer activity against acute myeloid leukemia. (S)-BI 2536 can be used for the research of acute myeloid leukemia.
-
PLK1-IN-16
0 ImagesCat. No.: HY-181051CAS No.: 3068378-51-5PLK1-IN-16 is a selective polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.25 nM. PLK1-IN-16 exhibits lower inhibitory potency against PLK2 and PLK3, induces G2 phase cell cycle arrest, induces apoptosis, and exhibits antiproliferative activity against tumor cells. PLK1-IN-16 can be stable under simulated gastric acid environmental conditions, and acceptable CYP 450 inhibition. PLK1-IN-16 can be used for the study of triple-negative breast cancer (TNBC), breast cancer, leukemia.
-
PLK1-IN-17
0 ImagesCat. No.: HY-184863CAS No.: 1034617-66-7PLK1-IN-17 is a potent PLK1 inhibitor with an IC50 of 2 nM. PLK1-IN-17 shows high selectivity for PLK2 and CDK2/A, moderate selectivity for PLK3, only weak activity against CK2, FLT3 and NEK6, and no activity against PDGFR, ALK and another 37 kinases. PLK1-IN-17 inhibits the proliferation of ovarian cancer cells and can be used in ovarian cancer-related research.
-
PLHSpT
0 ImagesCat. No.: HY-187593CAS No.: 1186496-84-3PLHSpT is an inhibitor of the Polo-box domain (PBD) of Polo-like kinase 1 (Plk1), with an IC50 of 36 μM. It binds to the PB1-PB2 cleft of the Plk1 PBD to block its interaction with phosphoprotein substrates, thereby inducing mitotic arrest and apoptosis in tumor cells. PLHSpT exerts antiglioma effects when delivered via liposomes, and it is applicable to research on glioblastoma multiforme and other human cancers.
-
IIP0943
0 ImagesCat. No.: HY-172677CAS No.: 3040106-93-9IIP0943 is a selective inhibitor of PLK1 (polo-like kinase 1), with an IC50 of 5.1 nM for PLK1. In addition, IIP0943 exhibits antiproliferative activity against HCT116 cells, with an IC50 of 0.22 µM. These results suggest that IIP0943 holds promise for research in the field of cancer therapeutics.
