Polo-like Kinases (PLKs) are a family of highly conserved serine/threonine protein kinases that are essential for a variety of biological functions, including cell division and mitosis checkpoint regulation. Five PLKs (PLK 1-5) play a variety of roles in DNA damage response, intra-S-phase and G2/M checkpoints, spindle formation, and centrosome dynamics in mammals.
PLKs are distinguished by their Polo-box domain, which mediates protein interactions. Depending on the biological context, they are also regulated by transcription, proteolysis, and phosphorylation. PLKs are now understood to function in differentiated cells and link cell division to developmental processes.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V115339 | PLK4-IN-5 | PLK4-IN-5 (compound 5f) is a PLK4 inhibitor (IC50 = 0.8 nM). | |
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V115581 | PLK4-IN-6 | PLK4-IN-6 (compound C05) is a PLK4 inhibitor (IC50 < 0.1 nM). | |
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V110858 | PLK4-IN-7 | PLK4-IN-7 is a highly selective, orally effective PLK4 inhibitor with an IC50 value of 7.9 nM. | |
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V112503 | PMV6-PEG4-BI2536 | PMV6-PEG4-BI2536 is a p53-Y220C-PLK1 bifunctional compound consisting of a high-affinity p53-Y220C mutant binder (Kd ≈ 2.5 nM) and a potent PLK1 kinase inhibitor (IC50 = 0.83 nM). | |
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V109335 | POI ligand-3 | POI ligand-3 (compound 4j) is a peptide PLK1 PBD inhibitor. | |
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V109328 | POI ligand-4 | 1403265-80-4 | POI ligand-4 is a PLK1 ligand that can be used to synthesize PROTACs, such as PROTAC PLK1 degrader-3. |
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V109907 | PROTAC PLK1 Degrader-2 | PROTAC PLK1 Degrader-2 (compound NC1) is a PLK1 PROTAC degrader with a Kd value of 6.06 μM. | |
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V109994 | PROTAC PLK1 Degrader-3 | 3074520-74-1 | PROTAC PLK1 degrader-3 (compound DD-1) is a PLK1 PROTAC degrader based on the N-deglycosylation pathway with a Kd value of 2.2 μM. |
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V1579 | Ro3280 (Ro5203280) | 1062243-51-9 | RO3280 (also known as Ro-5203280; RO 3280; Ro5203280; RO-3280) is a novel, potent and highly selective inhibitor of Polo-like kinase 1 (PLK1) with potential anticancer activity. |
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V144376 | RP-1664 | 2980682-00-4 | RP-1664 is a highly selective, orally effective PLK4 inhibitor with an IC50 value of 3 nM. |
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V1581 | SBE 13 HCl | 1052532-15-6 | SBE 13 HCl (SBE13; SBE-13), the hydrochloride salt of SBE13, is a novel, potent and selective Polo-like Kinase 1 (PLK1) inhibitor with potential antineoplastic activity. |
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V4581 | TAK-960 | 1137868-52-0 | TAK-960 (TAK960) is a novel, investigational, orally bioavailable, and selective inhibitor of polo-like kinase 1 (PLK1) with anticancer activity. |
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V4582 | TAK-960 dihydrochloride | 1137868-52-0 | TAK-960 DiHCl, the dihydrochloride salt of TAK960, is an orally bioavailable, potent, and selective PLK1 polo-like kinase 1 (PLK1) inhibitor with anIC50of 0.8 nM at 10 μM ATP. |
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V35228 | TAK-960 hydrochloride | 1137868-96-2 | TAK-960 HCl is a potent, orally bioavailable, selective polo-like kinase 1 (PLK1) inhibitor (antagonist) with IC50 of 0.8 nM. |
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V35229 | TAK-960 monohydrochloride | 2108449-45-0 | TAK-960 mono HCl is a potent, orally bioavailable, selective polo-like kinase 1 (PLK1) inhibitor (antagonist) with IC50 of 0.8 nM. |
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V104023 | TTK/PLK1-IN-1 | 1817791-70-0 | TTK/PLK1-IN-1 (Formula I) is an inhibitor of threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1) with IC50 of 7 nM and 72 nM, respectively. |
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V109917 | Y207–5465 | 667404-66-2 | Y207–5465 is a highly effective and selective PLK2 inhibitor with an IC50 value of 584.3 nM. |
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V79151 | YLT-11 | YLT-11 is a specific and orally bioactive PLK4 inhibitor (antagonist) with Kds of >10000, 653, >10000 and 5.2 nM for PLK1, PLK2, PLK3 and PLK4 respectively. | |
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V1574 | Volasertib (BI 6727) | 755038-65-4 | Volasertib (formerly also known as BI6727, BI-6727, BI 6727) is a novel and highly potent dihydropteridinone-based Plk1 (polo-like kinase 1) inhibitor with potential antineoplastic activity. |
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V4268 | Rigosertib (ON-01910) | 592542-59-1 | Rigosertib (formerly also known as ON-01910) is a novel, potent and non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. |