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PLK1 Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
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). Selective
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. Selective PLK1, IC50: 200 pM
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. Selective PLK1, IC50: 0.87 nM
S2898 MLN0905 MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM. Selective PLK1, IC50: 2 nM
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. Selective PLK1, IC50: 2 nM
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. Selective PLK1, Ki: 2.2 nM
S7248 Ro3280 RO3280 (Ro5203280) is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM. Selective PLK1, IC50: 3 nM
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. Selective PLK1, IC50: 9 nM
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. Selective Plk1 PBD, IC50: 4.8 μM
S1485 HMN-214 HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1. Selective
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. Pan PLK1, IC50: 0.83 nM
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. Pan PLK1, IC50: 2.2 nM