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Catalog No. Product Name Information Product Use Citations Product Validations
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.
Science, 2021, 371(6535)eabc5386
Nat Commun, 2021, 12(1):5356
Proc Natl Acad Sci U S A, 2021, 118(34)e2108145118
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.
Elife, 2021, 10e70715
Immun Inflamm Dis, 2021, 10.1002/iid3.458
Mol Cell, 2020, 79(1):191-198.e3
S1485 HMN-214 HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.
Exp Mol Med, 2020, 10.1038/s12276-020-00537-z
Stem Cells Dev, 2019, 28(7):438-453
Oncotarget, 2017, 8(58):97928-97940
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. Phase 1.
Cell Rep, 2021, 36(12):109740
Cancer Discov, 2021, candisc.1540.2020
Int J Radiat Oncol Biol Phys, 2021, S0360-3016(21)00203-0
S2235 Volasertib (BI 6727) Volasertib (BI 6727) 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.
Science, 2021, 371(6535)eabc5386
Mol Cell, 2021, S1097-2765(20)30946-1
Nat Commun, 2021, 12(1):5356
S2758 Wortmannin (KY 12420) Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) 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.
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
Adv Sci (Weinh), 2021, e2004303
J Extracell Vesicles, 2021, 10(8):e12091
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
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.
S7248 Ro3280 RO3280 (Ro5203280) is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.
J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096
Oncotarget, 2018, 9(47):28731-28744
J Cell Mol Med, 2017, 21(4):758-767
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.
Theranostics, 2021, 11(19):9571-9586
Cell Res, 2019, 29(9):725-738
Sci Rep, 2018, 8(1):3521
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.
Cell Death Dis, 2021, 12(7):640
J Cell Mol Med, 2020, 10.1111/jcmm.14996
Cancer Med, 2019, 8(14):6476-6484
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.
PLoS Pathog, 2021, 17(7):e1009764
Reprod Biol Endocrinol, 2021, 19(1):162
Sci Adv, 2020, 6(29):eaba1941
S7837New Centrinone (LCR-263) Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM.
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.
Science, 2021, 371(6535)eabc5386
Nat Commun, 2021, 12(1):5356
Proc Natl Acad Sci U S A, 2021, 118(34)e2108145118
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.
Elife, 2021, 10e70715
Immun Inflamm Dis, 2021, 10.1002/iid3.458
Mol Cell, 2020, 79(1):191-198.e3
S1485 HMN-214 HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.
Exp Mol Med, 2020, 10.1038/s12276-020-00537-z
Stem Cells Dev, 2019, 28(7):438-453
Oncotarget, 2017, 8(58):97928-97940
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. Phase 1.
Cell Rep, 2021, 36(12):109740
Cancer Discov, 2021, candisc.1540.2020
Int J Radiat Oncol Biol Phys, 2021, S0360-3016(21)00203-0
S2235 Volasertib (BI 6727) Volasertib (BI 6727) 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.
Science, 2021, 371(6535)eabc5386
Mol Cell, 2021, S1097-2765(20)30946-1
Nat Commun, 2021, 12(1):5356
S2758 Wortmannin (KY 12420) Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) 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.
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
Adv Sci (Weinh), 2021, e2004303
J Extracell Vesicles, 2021, 10(8):e12091
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
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.
S7248 Ro3280 RO3280 (Ro5203280) is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.
J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096
Oncotarget, 2018, 9(47):28731-28744
J Cell Mol Med, 2017, 21(4):758-767
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.
Theranostics, 2021, 11(19):9571-9586
Cell Res, 2019, 29(9):725-738
Sci Rep, 2018, 8(1):3521
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.
Cell Death Dis, 2021, 12(7):640
J Cell Mol Med, 2020, 10.1111/jcmm.14996
Cancer Med, 2019, 8(14):6476-6484
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.
PLoS Pathog, 2021, 17(7):e1009764
Reprod Biol Endocrinol, 2021, 19(1):162
Sci Adv, 2020, 6(29):eaba1941
S7837New Centrinone (LCR-263) Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM.
S7837New Centrinone (LCR-263) Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM.
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