| 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 |
