Polo-like Kinase (PLK) Inhibitor

KHS101 is a blood-brain barrier-penetrant anticancer agent that primarily functions by inhibiting HSPD1 (IC₅₀ = 14.4 μM) and TACC3 across different cellular backgrounds. KHS101 promotes the aggregation of HSPD1 with client proteins, destabilizes TACC3, and reduces the levels of TACC3, Aurora A and PLK1. KHS101 induces autophagy, apoptosis, cell cycle exit and neuronal differentiation; it suppresses cancer cell growth, motility, EMT and stemness; it also impairs mitochondrial bioenergetics and glycolysis in glioblastoma cells. KHS101 can be used in research related to glioblastoma multiforme and breast cancer.

PLK1-IN-15 (Compound 7n) is a PLK1 inhibitor (IC₅₀: 38.5 nM). PLK1-IN-15 exhibits antiproliferative activity against HepG2, Huh7, H1299 and A549 cells (IC₅₀: 2.03, 2.08, 4.79 and 17.11 μM, respectively). PLK1-IN-15 induces cell cycle arrest at the G2/M phase and apoptosis, and has anticancer activity.

BTO-1 is a Polo-like kinase (Plk) inhibitor. BTO-1 is primarily used for phosphorylation and dephosphorylation applications.

Salicylate choline is an orally active derivative of Aspirin (acetylsalicylic acid) (HY-14654). Salicylate choline significantly reduces IL-1β, IL-6, TNF-α and IL-10 levels in cells. Salicylate choline enhances the anti-tumor activity of the CRM1 inhibitor Selinexor (KPT-330) (HY-17536) through inducing S-phase cell cycle arrest and impairing DNA damage repair. Salicylate choline combined with Selinexor demonstrates excellent anti-tumor efficacy in mice xenograft model harboring JeKo-1 cells. Salicylate choline can be used for the study of rheumatic diseases, inflammation and cancer.

Wortmannin (Standard) is the analytical standard of Wortmannin. This product is intended for research and analytical applications. Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively.

Plk4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Plk4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

BI 2536 (GMP) is BI 2536 (HY-50698) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BI 2536 is a dual PLK1 and BRD4 inhibitor with IC₅₀s of 0.83 and 25 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription.

Plk2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Plk2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

PLK1/p38γ-IN-1(compound 14) is a multitarget inhibitors ofPLK1andp38γ. PLK1/p38γ-IN-1inhibits the growth of human hepatocellular carcinoma and hepatoblastoma cells in vitro.

MCC1019 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.

PLK4 Human Pre-designed siRNA Set A contains three designed siRNAs for PLK4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

DAP-81 is an inhibitory agent targeting Polo-like kinases (Plks), a class of evolutionarily conserved serine/threonine kinases. DAP-81 dose-dependently increases the number of monopolar spindles in treated cells. High-resolution live-cell microscopy revealed that Plk activity is required for the assembly and maintenance of bipolar mitotic spindles. Plk inhibition destabilizes centromeric microtubules while stabilizing other spindle microtubules, leading to the formation of monopolar spindles. Further testing of compounds based on "privileged scaffolds" such as the DAP scaffold may lead to the discovery of new cell division probes and anti-microtubule agents.

NL13 is a Polo-like kinase 4 (PLK4) inhibitor with an IC₅₀ value of 2.32 μM. NL13 can inhibit the viability of PC3 and DU145 prostate cancer cells, with IC₅₀ values of 3.51 μM and 2.53 μM, respectively. NL13 can lead to the inactivation of the AKT signaling pathway by downregulating CCNB1/CDK1, inducing G2/M cell cycle arrest, and triggering apoptosis through the cleavage of caspase-9/caspase-3. In prostate cancer mice, NL13 can inhibit tumor growth.

Plk1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Plk1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

ZNL-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 (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.

CZL-S092 is a PLK4 inhibitor with an IC₅₀ value of 0.9 nM and excellent selectivity over other PLK4 family members (PLK1, PLK2, and PLK3). CZL-S092 exhibits anti-neuroblastoma activity in vitro (IMR-32 cells, IC₅₀ = 1.143 μM). CZL-S092 inhibits cell migration and halts the cell cycle and induces apoptosis. CZL-S092 can be used in studies of various cancers including neuroblastoma cancer.

Allopole-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.

POI ligand-3 (Compound 4j) is a type of peptide-based PLK1 PBD inhibitor. POI ligand-3 can act as a target protein ligand and be used for the synthesis of PROTACs, such as PROTAC PLK1 Degrader-2 (HY-180989).

PLK1/PRC1-IN-1 (compound B4) is a PLK1/PRC1 protein complex formation inhibitor. PLK1/PRC1-IN-1 can be used in the study of non-small cell lung cancer (NSCLC) .