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PLK

PLK

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.

PLK related products

Structure Cat No. Product Name CAS No. Product Description
PLK4-IN-5 V115339 PLK4-IN-5 PLK4-IN-5 (compound 5f) is a PLK4 inhibitor (IC50 = 0.8 nM).
PLK4-IN-6 V115581 PLK4-IN-6 PLK4-IN-6 (compound C05) is a PLK4 inhibitor (IC50 < 0.1 nM).
PLK4-IN-7 V110858 PLK4-IN-7 PLK4-IN-7 is a highly selective, orally effective PLK4 inhibitor with an IC50 value of 7.9 nM.
PMV6-PEG4-BI2536 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).
POI ligand-3 V109335 POI ligand-3 POI ligand-3 (compound 4j) is a peptide PLK1 PBD inhibitor.
POI ligand-4 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.
PROTAC PLK1 Degrader-2 V109907 PROTAC PLK1 Degrader-2 PROTAC PLK1 Degrader-2 (compound NC1) is a PLK1 PROTAC degrader with a Kd value of 6.06 μM.
PROTAC PLK1 Degrader-3 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.
Ro3280 (Ro5203280) 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.
RP-1664 V144376 RP-1664 2980682-00-4 RP-1664 is a highly selective, orally effective PLK4 inhibitor with an IC50 value of 3 nM.
SBE 13 HCl 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.
TAK-960 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.
TAK-960 dihydrochloride 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.
TAK-960 hydrochloride 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.
TAK-960 monohydrochloride 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.
TTK/PLK1-IN-1 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.
Y207–5465 V109917 Y207–5465 667404-66-2 Y207–5465 is a highly effective and selective PLK2 inhibitor with an IC50 value of 584.3 nM.
YLT-11 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.
伏拉塞替 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.
瑞格色替 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.
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