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Cell Cycle/Checkpoint PLK

PLK

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.
Cat No. product name
T0973 Pyridoxine Pyridoxine is the 4-methanol form of vitamin B6 and is converted to pyridoxal 5-phosphate in the body. Although pyridoxine and vitamin B6 are still frequently u...
T2271 SBE 13 hydrochloride SBE13 hydrochloride is an effective and specific PLK1 inhibitor (IC50: 0.2 nM); no inhibition om Aurora A kinase, Plk2/3.
T2438 HMN214 HMN-214(IVX214) is a potent PLK1 inhibitor with an average IC50 of 0.12 μM.
T2634 RO 3280 Ro3280 is an effective, specific inhibitor of PLK1(IC50=3, Kd=0.09 nM).
T2704 MLN0905 MLN0905 is an effective PLK1 inhibitor(IC50=2 nM).
T6019 VolasertibHOT Volasertib (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).
T6173 BI 2536HOT BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.
T6247 NMS-P937 NMS-P937 (NMS1286937), an oral, specific Polo-like Kinase 1 (PLK1) inhibitor, is with IC50 of 2 nM. The specificity of NMS-P937 forPLK1 is 5000-fold higher ove...
T6282 GSK461364 GSK461364(Ki=2.2 nM) inhibits purified Plk1 .The specificity of GSK461364 for Plk1 is more than 1000-fold over Plk2/3.
T7200 TAK-960 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.
T5818 ON-01910 Rigosertib, a non-ATP-competitive inhibitor of PLK1(IC50=9 nM), exhibits 30-fold higher specificity activity over Plk2 and no effect on Plk3.
T16559 Poloxime Poloxime is a hydrolysis product of poloxin and is a non-ATP-competitive Plk1 inhibitor. It also has moderate Plk1 inhibitory activity.
T16560 Poloxin Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor. It targets the polo-box domain (IC50: appr 4.8 μM).
T16750 Rigosertib Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 (IC50: 9 nM). Rigosertib is a multi-kinase inhibitor and a selective anti-cancer agent, whic...
T17008 TC-S 7005 TC-S 7005 is an inhibitor of Polo-like kinases (IC50s: 4 nM, 24 nM and 214 nM for Plk2, Plk3, and Plk1, respectively).
TN3247 7-O-Prenylscopoletin 7-O-Prenylscopoletin and cedrelopsin show high antiproliferative activities against cancer cell lines.
Pyridoxine
T0973CAS 65-23-6
Pyridoxine is the 4-methanol form of vitamin B6 and is converted to pyridoxal 5-phosphate in the body. Although pyridoxine and vitamin B6 are still frequently u...
SBE 13 hydrochloride
T2271CAS 1052532-15-6
SBE13 hydrochloride is an effective and specific PLK1 inhibitor (IC50: 0.2 nM); no inhibition om Aurora A kinase, Plk2/3.
HMN214
T2438CAS 173529-46-9
HMN-214(IVX214) is a potent PLK1 inhibitor with an average IC50 of 0.12 μM.
RO 3280
T2634CAS 1062243-51-9
Ro3280 is an effective, specific inhibitor of PLK1(IC50=3, Kd=0.09 nM).
MLN0905
T2704CAS 1228960-69-7
MLN0905 is an effective PLK1 inhibitor(IC50=2 nM).
Volasertib HOT
T6019CAS 755038-65-4
Volasertib (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).
BI 2536 HOT
T6173CAS 755038-02-9
BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.
NMS-P937
T6247CAS 1034616-18-6
NMS-P937 (NMS1286937), an oral, specific Polo-like Kinase 1 (PLK1) inhibitor, is with IC50 of 2 nM. The specificity of NMS-P937 forPLK1 is 5000-fold higher ove...
GSK461364
T6282CAS 929095-18-1
GSK461364(Ki=2.2 nM) inhibits purified Plk1 .The specificity of GSK461364 for Plk1 is more than 1000-fold over Plk2/3.
TAK-960
T7200CAS 1137868-52-0
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.
ON-01910
T5818CAS 592542-60-4
Rigosertib, a non-ATP-competitive inhibitor of PLK1(IC50=9 nM), exhibits 30-fold higher specificity activity over Plk2 and no effect on Plk3.
Poloxime
T16559CAS 17302-61-3
Poloxime is a hydrolysis product of poloxin and is a non-ATP-competitive Plk1 inhibitor. It also has moderate Plk1 inhibitory activity.
Poloxin
T16560CAS 321688-88-4
Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor. It targets the polo-box domain (IC50: appr 4.8 μM).
Rigosertib
T16750CAS 592542-59-1
Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 (IC50: 9 nM). Rigosertib is a multi-kinase inhibitor and a selective anti-cancer agent, whic...
TC-S 7005
T17008CAS 1082739-92-1
TC-S 7005 is an inhibitor of Polo-like kinases (IC50s: 4 nM, 24 nM and 214 nM for Plk2, Plk3, and Plk1, respectively).
7-O-Prenylscopoletin
TN3247CAS 13544-37-1
7-O-Prenylscopoletin and cedrelopsin show high antiproliferative activities against cancer cell lines.