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PLK

Isoform-selective Products

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PLK Products

All (17)
PLK Inhibitors (17)
New PLK Products

Catalog No.	Product Name	Information	Product Use Citations
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.	Nature, 2024, 10.1038/s41586-024-07990-0 Nat Commun, 2024, 15(1):451 Nat Commun, 2024, 15(1):4926
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.	Leukemia, 2024, 38(5):969-980 Clin Transl Med, 2024, 14(5):e1703 Clin Transl Med, 2024, 14(5):e1703
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.	Nat Commun, 2024, 15(1):2810 Haematologica, 2024, 109(6):1726-1740 Cell Rep, 2024, 43(8):114510
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.	Nat Commun, 2024, 15(1):2089 Environ Mol Mutagen, 2024, 10.1002/em.22604 Cancer Cell, 2022, 40(7):754-767.e6
S2193	GSK461364	GSK461364 (GSK461364A) inhibits purified Plk1 with K_i 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.	EMBO Mol Med, 2024, 10.1038/s44321-024-00060-y Clin Transl Med, 2024, 14(5):e1703 Clin Transl Med, 2024, 14(5):e1703
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.	JCI Insight, 2024, 9(8)e173205 Cancers (Basel), 2023, 15(9)2589 J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096
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 Nat Commun, 2023, 14(1):6505
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.	Cell Rep, 2024, 43(8):114510
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.	Nature, 2024, 10.1038/s41586-024-07990-0 Nat Commun, 2024, 15(1):451 Nat Commun, 2024, 15(1):4926
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.	Leukemia, 2024, 38(5):969-980 Clin Transl Med, 2024, 14(5):e1703 Clin Transl Med, 2024, 14(5):e1703
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.	Nat Commun, 2024, 15(1):2810 Haematologica, 2024, 109(6):1726-1740 Cell Rep, 2024, 43(8):114510
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.	Nat Commun, 2024, 15(1):2089 Environ Mol Mutagen, 2024, 10.1002/em.22604 Cancer Cell, 2022, 40(7):754-767.e6
S2193	GSK461364	GSK461364 (GSK461364A) inhibits purified Plk1 with K_i 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.	EMBO Mol Med, 2024, 10.1038/s44321-024-00060-y Clin Transl Med, 2024, 14(5):e1703 Clin Transl Med, 2024, 14(5):e1703
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.	JCI Insight, 2024, 9(8)e173205 Cancers (Basel), 2023, 15(9)2589 J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096
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 Nat Commun, 2023, 14(1):6505
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.	Cell Rep, 2024, 43(8):114510

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