2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Polo-like Kinase (PLK)

Polo-like Kinase (PLK)

Polo-like Kinase (PLK)

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Polo-like Kinases (PLKs) are a group of highly conserved serine/threonine protein kinases that play a key role in processes such as cell division and checkpoint regulation of mitosis. In mammals, five PLKs (PLK 1-5) encompass diverse roles in centrosome dynamics, spindle formation, intra S-phase and G2/M checkpoints, and DNA damage response.

PLKs are characterized by their Polo-box domain, which mediates protein interactions. They are additionally controlled by phosphorylation, proteolysis, and transcription, depending on the biological context. PLKs are now recognized to link cell division to developmental processes and to function in differentiated cells.

Polo-like Kinase (PLK) Isoform Specific Products:

Polo-like Kinase (PLK) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-149100
    PLK1-IN-6
    		Inhibitor
    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.
    PLK1-IN-6
  • HY-124761
    Poloppin
    		Inhibitor
    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) (Kd= 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.
    Poloppin
  • HY-143471
    PLK1/BRD4-IN-1
    		Inhibitor
    PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity.
    PLK1/BRD4-IN-1
  • HY-158031
    PLK1/BRD4-IN-5
    		Inhibitor
    PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3  nM and 60.8  nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research.
    PLK1/BRD4-IN-5
  • HY-120279A
    CFI-400437
    		Inhibitor
    CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC50 of 0.6 nM).
    CFI-400437
  • HY-115589
    YLT-11
    		Inhibitor
    YLT-11 is a potent, selective and orally active PLK4 inhibitor with Kd values of >10000, 653, >10000, 5.2 nM for PLK1, PLK2, PLK3, PLK4, respectively. YLT-11 shows antiproliferative activity. YLT-11 induces Apoptosis.html" class="link-product" target="_blank">Apoptosis and cell cycle arrest at G2/M phase. YLT-11 show anticancer activity.
    YLT-11
  • HY-134775A
    PLK4-IN-3
    		Inhibitor
    PLK4-IN-3 is a less active absolute stereochemistry of PLK4-IN-1. PLK4-IN-1 is a PLK4 inhibitor, with an IC50 of 0.65 μM.
    PLK4-IN-3
  • HY-149912
    CZS-241
    		Inhibitor
    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
  • HY-148974
    PLK1-IN-5
    		Inhibitor
    PLK1-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-5
  • HY-146792
    PLK1-IN-4
    		Inhibitor
    PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma.
    PLK1-IN-4
  • HY-139652
    PLK1-IN-2
    		Inhibitor
    PLK1-IN-2 is a PLK1 kinase inhibitor with an IC50 value of 0.384 μM.
    PLK1-IN-2
  • HY-15160C
    TAK-960 monohydrochloride
    		Inhibitor
    TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
    TAK-960 monohydrochloride
  • HY-161046
    PLK1-IN-8
    		Inhibitor
    PLK1-IN-8 (compound TE6) is a PLK1 inhibitor, and inhibits cell proliferation by blocking the cell cycle at G2 phase. PLK1-IN-8 shows anticancer activity in vivo.
    PLK1-IN-8
  • HY-156336
    PLK1-IN-7
    		Inhibitor
    PLK1-IN-7 (compound 30e) is a potent PLK1 inhibitor, with an IC50 of 0.66 nM. PLK1-IN-7 exhibits antiproliferative and antitumor activities.
    PLK1-IN-7
  • HY-15160A
    TAK-960 hydrochloride
    		Inhibitor
    TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
    TAK-960 hydrochloride
  • HY-160624
    CD 10899
    		Inhibitor
    CD 10899 is a hydroxylated metabolite of Volasertib (HY-12137). CD 10899 is pharmacologically active against Polo-like kinase 1 (PLK1) (IC50: 6 nM). Volasertib is an orally active, highly potent and ATP-competitive PLK1 inhibitor. CD 10899 can be used for research of cancer.
    CD 10899
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Polo-like Kinase (PLK) Isoform Comparison

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