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Cell Cycle/Checkpoint Cell Cycle/CheckpointPLK
Polo-like kinase (PLK) is a highly conserved serine/threonine protein kinase with a highly homologous serine/threonine kinase domain at its N-terminus, which regulates PLK activity and subcellular dynamics at the C-terminus and targeted polo-box domain (PBD). There are many PLK family members, and there are four subtypes in the human body, namely PLK1, PLK2, PLK3, and PLK4, which play important roles in the regulation of various phases of the cell cycle.
Onvansertib
Cited
T62471034616-18-6
Onvansertib (NMS-1286937) is a PLK1 inhibitor (IC50=2 nM) with high selectivity and oral activity. Onvansertib has antitumor activity and inhibits tumor growth.
- $30
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CitedWortmannin Cited
T628319545-26-7
Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8 48 nM) that blocks autophagy.
- $32
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CitedVolasertib Cited
T6019755038-65-4
Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2 PLK3 (IC50s: 5 56 nM).
- $39
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CitedOcifisertib（CFI-400945 free base）
T73841338806-73-7
Ocifisertib (CFI-400945 free base) is a potent, selective and orally active inhibitor of polo-like kinase 4 (PLK4; Ki value 0.26 nM; IC50 value 2.8 nM).
- $38
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(E/Z)-Rigosertib sodium
T60701225497-78-8
ON-01910 is a non-ATP-competitive PLK1 inhibitor(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.It is a synthetic benzyl styryl sulfone analogue with potential antineoplastic activity.
- $34
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GSK461364 Cited
T6282929095-18-1
GSK461364 (GSK461364A)(Ki=2.2 nM) inhibits purified Plk1 .The specificity of GSK461364 for Plk1 is more than 1000-fold over Plk2 3.
- $31
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CitedBI 2536 Cited
T6173755038-02-9
BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.
- $38
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CitedPoloxin-2
T25969321695-37-8In house
Poloxin-2 is a potent and selective Plk1 PBD inhibitor with anti-tumour activity that reduces the protein level of Plk1 in HeLa cells.
- $350
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Dihydrobaicalein
TN384835683-17-1
Dihydrobaicalein is a natural product from Scutellaria baicalensis, a PLK1 inhibitor (IC50:6.3 μM).Dihydrobaicalein inhibits VRK2 and PLK2.
- $195
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Rigosertib
T16750592542-59-1
Rigosertib (ON-01910) is a selective, non-ATP-competitive PLK1 inhibitor (IC50: 9 nM) and multi-kinase inhibitor. As a selective anti-cancer agent, Rigosertib induces apoptosis by inhibiting the PI3 kinase Akt pathway, promotes histone H2AX phosphorylation, and induces G2 M arrest in the cell cycle.
- $34
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Plogosertib
T713991137212-79-3In house
Plogosertib (CYC140) is an orally active, selective, potent, and ATP-competitive PLK1 inhibitor with an IC50 value of 3 nM.Plogosertib exhibits antiproliferative and anticancer activity and can be used for the study of solid and hematologic tumors. and hematologic tumors.
- $228
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Mps1-IN-2
T18391228817-38-6
Mps1-IN-2 is a potent, selective, and ATP-competitive inhibitor of both Mps1 and Plk1.
- $34
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Centrinone
T149271798871-30-3
Centrinone (LCR-263) (LCR-263) is a reversible inhibitor of polo-like kinase 4 (PLK4; Ki:0.16 nM).
- $56
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3MB-PP1
T21678956025-83-5In house
3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor. In cells expressing analog-sensitive Plk1 alleles, 3MB-PP1 blocks mitotic progression and cell division arise by targeting Plk1. 3MB-PP1 specifically inhibits analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase with IC50 of 2 μM. 3MB-PP1 can be used for the research of cell division and hypha formation of Candida albicans.
- $48
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MLN0905
T27041228960-69-7
MLN0905 (PLK1 Inhibitor) is an effective PLK1 inhibitor(IC50=2 nM).
- $55
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TAK-960
T72001137868-52-0
TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively.
- $58
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HMN-214
T2438173529-46-9
HMN-214 (IVX-214) is a potent PLK1 inhibitor with an average IC50 of 0.12 μM.
- $34
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Cyclapolin 9
T2270040533-25-3
Cyclapolin 9 is a selective, potent, and ATP-competitive inhibitor of polo-like kinase 1 (PLK1) with an IC50 of 500 nM, and has not shown activity against other kinases.
- $93
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Ro3280
T26341062243-51-9
Ro3280 (Ro5203280) is an effective, specific inhibitor of PLK1(IC50=3, Kd=0.09 nM).
- $55
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GW843682X
T15454660868-91-7
GW843682X (GW843682) is a selective and ATP-competitive inhibitor of PLK1 and PLK3 (IC50s = 2.2 nM and 9.1 nM).
- $32
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LFM-A13 Cited
T6217244240-24-2
LFM-A13（IC50=2.5 μM）, a specific Bruton's tyrosine kinase (BTK), is more than 100-fold specificity than other protein kinases, such as JAK1, JAK2, HCK, EGFR, and IRK.
- $30
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CitedPHA-680632
T6338398493-79-3
PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2 3.
- $39
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AAPK-25
T102152247919-28-2
AAPK-25 is a potent and selective Aurora PLK dual inhibitor with anti-tumor activity, causing mitotic delay and arresting cells in prometaphase, followed by increased apoptosis. It targets Aurora-A -B -C with Kd values ranging from 23-289 nM.
- $87
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Centrinone-B
T149261798871-31-4In house
Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor with a Ki of 0.59 nM.
- $199
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HMN-176
T3643173529-10-7
HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1).
- $36
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(1E)-CFI-400437 dihydrochloride
T222881247000-76-5
(1E)-CFI-400437 dihydrochloride (CFI-400437 dihydrochloride) is a selective and potent polo-like kinase 4 (PLK4) inhibitor.
- $80
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Poloxin
T16560321688-88-4
Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor targeting the polo-box domain (IC50: appr 4.8 μM).
- $32
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TC-S 7005
T170081082739-92-1
TC-S 7005 is an effective inhibitor of Polo-like kinases (IC50s: 214 nM, 4 nM and 24 nM for Plk1, Plk2, and Plk3).
- $52
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5-ETHYL-4,5,6,7-TETRAHYDRO-THIAZOLO[5,4-C]PYRIDIN-2-YLAMINE
T891217899-49-9
5-ETHYL-4,5,6,7-TETRAHYDRO-THIAZOLO[5,4-C]PYRIDIN-2-YLAMINE targets PLK1.
- $31
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Rigosertib sodium
T5818592542-60-4
Rigosertib sodium (ON-01910), a non-ATP-competitive inhibitor of PLK1(IC50=9 nM), exhibits 30-fold higher specificity activity over Plk2 and no effect on Plk3.
- $33
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ON1231320
T196641312471-39-8
ON1231320 (GBO-006) is a Polo-like kinase 2 (PLK2) inhibitor.
- $40
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T521
T28904891020-54-5In house
T521 is a selective inhibitor of the PBD of Plk1 and shows no inhibitory effect on Plk2 and Plk3.
- $410
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SBE13 Hydrochloride
T22711052532-15-6
SBE13 Hydrochloride (SBE 13 HCl) is an effective and specific PLK1 inhibitor (IC50: 0.2 nM); no inhibition om Aurora A kinase, Plk2/3.
- $29
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7-O-Prenylscopoletin
TN324713544-37-1
7-O-Prenylscopoletin and cedrelopsin show high antiproliferative activities against cancer cell lines.
- $440
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Poloxime
T1655917302-61-3
Poloxime is a hydrolysis product of poloxin and is a non-ATP-competitive Plk1 inhibitor. It also has moderate Plk1 inhibitory activity.
- $39
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