PLK

Isoform-selective Products

Signaling Pathway

PLK Signaling Pathway

PLK Products

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  • PLK Inhibitors (17)
  • New PLK Products
Catalog No. Product Name Information Product Use Citations Product Validations
S2758 Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Nat Commun, 2024, 15(1):451
J Exp Med, 2023, 220(9)e20230054
Autophagy, 2023, 19(4):1164-1183
S1109 BI 2536 BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
Nature, 2023, 621(7978):415-422
Circulation, 2023, 148(19):1459-1478
Nat Commun, 2023, 14(1):6088
S2235 Volasertib Volasertib is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3.
Mol Oncol, 2024, 10.1002/1878-0261.13610
Cancer Cell Int, 2024, 24(1):73
Eur J Pharmacol, 2024, 963:176229
S1362 Rigosertib (ON-01910) Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3.
Cancer Cell, 2022, 40(7):754-767.e6
Mater Today Bio, 2022, 17:100503
Cancers (Basel), 2022, 14(6)1575
S2193 GSK461364 GSK461364 (GSK461364A) inhibits purified Plk1 with Ki of 2.2 nM in a cell-free assay. It is more than 1000-fold selective against Plk2/3.
Sci Signal, 2022, 15(754):eabj4009
Cancers (Basel), 2022, 14(6)1575
Cancer Discov, 2021, candisc.1540.2020
S7255 Onvansertib (NMS-P937) Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed by apoptosis in cancer cell lines and inhibits tumor growth. Phase 1.
Am J Cancer Res, 2023, 13(2):623-637
Sci Rep, 2023, 13(1):16271
Nat Commun, 2022, 13(1):4261
S7720 SBE 13 HCl SBE 13 HCl is a potent and selective PLK1 inhibitor with IC50 of 200 pM, >4000-fold selectivity over Aurora A kinase, Plk2 and Plk3.
J Clin Invest, 2023, 133(21)e162129
J Clin Invest, 2023, 133(21)e162129
PLoS Pathog, 2021, 17(7):e1009764
S1485 HMN-214 HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.
Cancers (Basel), 2022, 14(6)1575
Exp Mol Med, 2020, 10.1038/s12276-020-00537-z
Stem Cells Dev, 2019, 28(7):438-453
S7248 Ro3280 RO3280 (Ro5203280) is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.
Cancers (Basel), 2023, 15(9)2589
J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096
Oncotarget, 2018, 9(47):28731-28744
S7552 CFI-400945 CFI-400945 is an orally active, potent and selective polo-like kinase 4(PLK4) inhibitor with Ki value of 0.26 nM.
Radiat Oncol, 2024, 19(1):24
Nat Commun, 2023, 14(1):6505
Cell Death Discov, 2023, 9(1):49
S2898 MLN0905 MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.
Science Bulletin, 2018, 10.1016/j.scib.2018.09.024
Hepatology, 2017, 10.1002/hep.29236
S5893 Poloxin Poloxin is a non-ATP competitive Polo-like Kinase 1 polo-box domain (Plk1 PBD) inhibitor with an apparent IC50 of 4.8 μM. Poloxin's IC50 values against the PBDs of Plk2 and Plk3 as Plk1 are approximately 4-fold and 11-fold higher, respectively in fluorescence polarization assays.
Nat Commun, 2023, 14(1):355
S1239 TAK-960 TAK-960 is a novel, investigational, orally bioavailable, potent, and selective PLK1 inhibitor that has shown activity in several tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1).
S2880 GW843682X GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ~30 other kinases.
S5807 HMN-176 HMN-176 is an active metabolite of HMN-214, which has a potent antitumor activity in mouse xenograft models. HMN-176 effectively inhibits PLK-1 by interference with its normal subcellular spatial distribution at centrosomes and along the cytoskeletal structure.
S7837 Centrinone (LCR-263) Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM.
S8342 ON1231320 ON1231320 (7ao), an arylsulfonyl pyrido-pyrimidinone, is a highly specific inhibitor of polo like kinase 2 (PLK2). It also blocks tumor cell cycle progression in the G2/M phase in mitosis and causes apoptosis.
S2758 Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Nat Commun, 2024, 15(1):451
J Exp Med, 2023, 220(9)e20230054
Autophagy, 2023, 19(4):1164-1183
S1109 BI 2536 BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
Nature, 2023, 621(7978):415-422
Circulation, 2023, 148(19):1459-1478
Nat Commun, 2023, 14(1):6088
S2235 Volasertib Volasertib is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3.
Mol Oncol, 2024, 10.1002/1878-0261.13610
Cancer Cell Int, 2024, 24(1):73
Eur J Pharmacol, 2024, 963:176229
S1362 Rigosertib (ON-01910) Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3.
Cancer Cell, 2022, 40(7):754-767.e6
Mater Today Bio, 2022, 17:100503
Cancers (Basel), 2022, 14(6)1575
S2193 GSK461364 GSK461364 (GSK461364A) inhibits purified Plk1 with Ki of 2.2 nM in a cell-free assay. It is more than 1000-fold selective against Plk2/3.
Sci Signal, 2022, 15(754):eabj4009
Cancers (Basel), 2022, 14(6)1575
Cancer Discov, 2021, candisc.1540.2020
S7255 Onvansertib (NMS-P937) Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed by apoptosis in cancer cell lines and inhibits tumor growth. Phase 1.
Am J Cancer Res, 2023, 13(2):623-637
Sci Rep, 2023, 13(1):16271
Nat Commun, 2022, 13(1):4261
S7720 SBE 13 HCl SBE 13 HCl is a potent and selective PLK1 inhibitor with IC50 of 200 pM, >4000-fold selectivity over Aurora A kinase, Plk2 and Plk3.
J Clin Invest, 2023, 133(21)e162129
J Clin Invest, 2023, 133(21)e162129
PLoS Pathog, 2021, 17(7):e1009764
S1485 HMN-214 HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.
Cancers (Basel), 2022, 14(6)1575
Exp Mol Med, 2020, 10.1038/s12276-020-00537-z
Stem Cells Dev, 2019, 28(7):438-453
S7248 Ro3280 RO3280 (Ro5203280) is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.
Cancers (Basel), 2023, 15(9)2589
J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096
Oncotarget, 2018, 9(47):28731-28744
S7552 CFI-400945 CFI-400945 is an orally active, potent and selective polo-like kinase 4(PLK4) inhibitor with Ki value of 0.26 nM.
Radiat Oncol, 2024, 19(1):24
Nat Commun, 2023, 14(1):6505
Cell Death Discov, 2023, 9(1):49
S2898 MLN0905 MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.
Science Bulletin, 2018, 10.1016/j.scib.2018.09.024
Hepatology, 2017, 10.1002/hep.29236
S5893 Poloxin Poloxin is a non-ATP competitive Polo-like Kinase 1 polo-box domain (Plk1 PBD) inhibitor with an apparent IC50 of 4.8 μM. Poloxin's IC50 values against the PBDs of Plk2 and Plk3 as Plk1 are approximately 4-fold and 11-fold higher, respectively in fluorescence polarization assays.
Nat Commun, 2023, 14(1):355
S1239 TAK-960 TAK-960 is a novel, investigational, orally bioavailable, potent, and selective PLK1 inhibitor that has shown activity in several tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1).
S2880 GW843682X GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ~30 other kinases.
S5807 HMN-176 HMN-176 is an active metabolite of HMN-214, which has a potent antitumor activity in mouse xenograft models. HMN-176 effectively inhibits PLK-1 by interference with its normal subcellular spatial distribution at centrosomes and along the cytoskeletal structure.
S7837 Centrinone (LCR-263) Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM.
S8342 ON1231320 ON1231320 (7ao), an arylsulfonyl pyrido-pyrimidinone, is a highly specific inhibitor of polo like kinase 2 (PLK2). It also blocks tumor cell cycle progression in the G2/M phase in mitosis and causes apoptosis.

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