Polo-like Kinase (PLK) Inhibitor

Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC₅₀ and a K_d of 145 nM and 12 nM for Mps1 and a K_d of 61 nM for Plk1.

PLK4-IN-1 is a spiro cyclopropyl indolinone compound and PLK4 inhibitor with inhibitory activity against Aurora A and Aurora B kinases .PLK4-IN-1 can be used for the research of cancer .

Cyclapolin 9 is a potent, selective and ATP-competitive polo-like kinase 1 (PLK1) inhibitor with an IC₅₀ of 500 nM. Cyclapolin 9 is inactive against other kinases.

(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC₅₀= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC₅₀s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity.

8012-3246 is a selective PLK2 inhibitor with an IC₅₀ of 774.5 nM. 8012-3246 suppresses GSK3β phosphorylation. 8012-3246 exhibits potent anticancer activity against colorectal cancer.

PLK1 Human Pre-designed siRNA Set A contains three designed siRNAs for PLK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

PLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC₅₀s of 0.059, 0.127 and 0.245 μM, respectively.

PLK1-IN-13 is a selective and orally active PLK1 inhibitor (IC₅₀: 0.27 nM). PLK1-IN-13 also inhibits PLK2 (IC₅₀: 12.72 nM) and PLK3 (IC₅₀: 4.12 nM). PLK1-IN-13 arrests cell at G2 phase, induces apoptosis and down-regulates the transcription of the proliferation-related oncogene c-MYC. PLK1-IN-13 inhibits tumor growth, and can be used for research of acute myeloid leukemia (AML).

PLK1-IN-6 is a potent and selective PLK1 inhibitor, with an IC₅₀ of 0.45 nM. PLK1-IN-6 shows significant anti-proliferative activities against cancer cells.

Dihydrobaicalein is a PLK1 Inhibitor with an IC₅₀ of 6.3 μM. Dihydrobaicalein also inhibits VRK2 and PLK2. Dihydrobaicalein is a natural product that can be isolated from Scutellaria scandens.

TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC₅₀ of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC₅₀s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.

PLK1-IN-11 (Cluster 4, 16953209) is a PLK1 inhibitor, with IC₅₀ of 1 μM. PLK1-IN-11 can be used in research on a variety of cancers, including pancreatic, ovarian, breast, and non-small cell lung carcinoma.

Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC₅₀=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (K_d= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors.

Poloxime, a hydrolysis product of poloxin, is a non-ATP-competitive Plk1 inhibitor, with moderate Plk1 inhibitory activity.

Y207–5465 is a potent and highly selective PLK2 inhibitor with an IC₅₀ value of 584.3 nM. Y207–5465 shows only limited anti-cancer activity in HT-29 and HCT-116 cells. Y207–5465 can be used in cancer research.

CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC₅₀=2.6 nM). CZS-241 inhibits TRKA with an IC₅₀ value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines.

CZS-241 hydrochloride is an orally active and selective inhibitor of Polo-like Kinase 4 (PLK4) (IC₅₀=2.6 nM). CZS-241 hydrochloride inhibits TRKA with an IC₅₀ value of 2.74 μM. CZS-241 hydrochloride induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 hydrochloride shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines.

SBE13 is a potent and selective Plk1 inhibitor, with an IC₅₀ of 200 pM; SBE13 poorly inhibits Plk2 (IC₅₀>66 μM) or Plk3 (IC₅₀=875 nM).

Ocifisertib hydrochloride (CFI-400945 hydrochloride) is the hydrochloride salt form of Ocifisertib (HY-12300). Ocifisertib hydrochloride is an orally active PLK4 inhibitor with a K_i and an IC₅₀ of 0.26 nM and 2.8 nM. Ocifisertib hydrochloride inhibits growth of various cancer cells, arrests cell cycles at G2/M phase, and induces apoptosis. Ocifisertib hydrochloride exhibits antitumor efficacy in mouse model.

ZSL-M028 is an orally active and selective Polo-like kinase 4 (PLK4) inhibitor with an IC₅₀ value of 1.1 nM. ZSL-M028 exhibits anti-tumor activity against TRIM37-amplified neuroblastoma, downregulates SAS6, upregulates FBXW5, induces G2-phase cell cycle arrest and apoptosis, activates the p53 signaling pathway, and inhibits tumor cell colony formation and migration. ZSL-M028 shows significant tumor growth inhibitory activity in the IMR-32 neuroblastoma xenograft model. ZSL-M028 can be used in neuroblastoma-related research.