Application | Comment | Organism |
---|---|---|
additional information | with respect to both substrate and ATP-site specificity, highest similarity is between PLK2 and PLK3, PLK1 is next most similar, and PLK4 is least similar | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
GST-tagged PLK1 (1-331) expressed in SF9 cells | Homo sapiens |
His-tagged PLK4 (1-269) expressed in Escherichia coli | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2-ol | selectivity profile of PLK2/4 over PLK1/3 | Homo sapiens | |
AG-013736 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
BAY 439006 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
BI 2536 | time-dependent inhibition; time-dependent inhibition; time-dependent inhibition of PLK1 | Homo sapiens | |
CHIR-258 | selectivity profile of PLK2/4 over PLK1/3; selectivity profile of PLK2/4 over PLK1/3 | Homo sapiens | |
CP 547632 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
GO 6976 | loses PLK1 activity by at least an order of magnitude, relative to staurosporine; loses PLK2 activity by at least an order of magnitude, relative to staurosporine; loses PLK3 activity by at least an order of magnitude, relative to staurosporine | Homo sapiens | |
H-1152 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
imatinib | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
LY294002 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
additional information | GO 6976 retains PLK4 activity | Homo sapiens | |
PP1 | - |
Homo sapiens | |
staurosporine | specific for PLK4 | Homo sapiens | |
SU11248 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
VX-680 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
Wortmannin | time-dependent irreversible inhibition with PLK1 | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0002 | - |
ATP | - |
Homo sapiens | |
0.0008 | - |
ATP | - |
Homo sapiens | |
0.001 | - |
ATP | - |
Homo sapiens | |
0.002 | - |
ATP | PLK2 | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O00444 | - |
- |
Homo sapiens | P53350 | - |
- |
Homo sapiens | Q9H4B4 | - |
- |
Homo sapiens | Q9NYY3 | - |
- |
Purification (Comment) | Organism |
---|---|
affinity purified | Homo sapiens |
on Ni2+ resin | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + Cdc25C | preferentially phosphorylates Ser 198 and 191 | Homo sapiens | ADP + phosphorylated Cdc25C | - |
? | |
ATP + cJun peptide | strong preference of PLK1 versus PLK2 and PLK3 | Homo sapiens | ADP + phosphorylated cJun peptide | - |
? | |
ATP + PLKtide | substrate corresponds to the consensus sequence for positions -7 to +6 supplemented with residues from Cdc25C for positions -23 to -8. PLK1 displays greatly enhanced activity and a strong preference for the residue corresponding to Ser198 in the optimized substrate | Homo sapiens | ADP + phosphorylated PLKtide | - |
? | |
ATP + PLKtide | substrate corresponds to the consensus sequence for positions -7 to +6 supplemented with residues from Cdc25C for positions -23 to -8. PLK2 displays greatly enhanced activity and a strong preference for the residue corresponding to Ser198 in the optimized substrate | Homo sapiens | ADP + phosphorylated PLKtide | - |
? | |
ATP + PLKtide | substrate corresponds to the consensus sequence for positions -7 to +6 supplemented with residues from Cdc25C for positions -23 to -8. PLK3 displays greatly enhanced activity and a strong preference for the residue corresponding to Ser198 in the optimized substrate | Homo sapiens | ADP + phosphorylated PLKtide | - |
? | |
ATP + TPSDSLIYDDGLS | - |
Homo sapiens | ADP + phosphorylated TPSDSLIYDDGLS | - |
? | |
additional information | consensus substrate sequences for PLK2 | Homo sapiens | ? | - |
? | |
additional information | consensus substrate sequences for PLK3 | Homo sapiens | ? | - |
? | |
additional information | consensus substrate sequences for PLK4 | Homo sapiens | ? | - |
? | |
additional information | expanded consensus substrate sequence for PLK1 | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Plk1 | - |
Homo sapiens |
Plk2 | - |
Homo sapiens |
Plk3 | - |
Homo sapiens |
PLK4 | - |
Homo sapiens |
Polo-like kinase 1 | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000001 | - |
BI 2536 | time-dependent inhibition | Homo sapiens | |
0.0000026 | - |
staurosporine | - |
Homo sapiens | |
0.0000034 | - |
GO 6976 | - |
Homo sapiens | |
0.0000042 | - |
AG-013736 | - |
Homo sapiens | |
0.000011 | - |
N-[4-({4-[(Z)-(5-methyl-1,2-dihydro-3H-pyrazol-3-ylidene)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide | - |
Homo sapiens | |
0.00012 | - |
CP 547632 | - |
Homo sapiens | |
0.00012 | - |
H-1152 | - |
Homo sapiens | |
0.00015 | - |
staurosporine | - |
Homo sapiens | |
0.00024 | - |
BAY 439006 | - |
Homo sapiens | |
0.0003 | - |
SU11248 | - |
Homo sapiens | |
0.00079 | - |
staurosporine | - |
Homo sapiens | |
0.00079 | - |
PP1 | - |
Homo sapiens | |
0.00085 | - |
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2-ol | - |
Homo sapiens | |
0.0012 | - |
staurosporine | - |
Homo sapiens | |
0.0014 | - |
CHIR-258 | - |
Homo sapiens | |
0.0015 | - |
Wortmannin | time-dependent irreversible inhibition | Homo sapiens | |
0.0022 | - |
imatinib | - |
Homo sapiens | |
0.0028 | - |
Wortmannin | - |
Homo sapiens | |
0.003 | - |
Wortmannin | - |
Homo sapiens | |
0.0061 | - |
LY294002 | - |
Homo sapiens | |
0.0075 | - |
LY294002 | - |
Homo sapiens | |
0.008 | - |
GO 6976 | - |
Homo sapiens | |
0.0093 | - |
SU11248 | - |
Homo sapiens | |
0.016 | - |
LY294002 | - |
Homo sapiens | |
0.016 | - |
GO 6976 | - |
Homo sapiens | |
0.018 | - |
imatinib | - |
Homo sapiens | |
0.019 | - |
GO 6976 | - |
Homo sapiens | |
0.02 | - |
Wortmannin | - |
Homo sapiens | |
0.02 | - |
LY294002 | - |
Homo sapiens | |
0.02 | - |
imatinib | - |
Homo sapiens | |
0.02 | - |
BI 2536 | - |
Homo sapiens | |
0.02 | - |
PP1 | - |
Homo sapiens | |
0.02 | - |
SU11248 | - |
Homo sapiens | |
0.02 | - |
BAY 439006 | - |
Homo sapiens | |
0.02 | - |
CP 547632 | - |
Homo sapiens | |
0.02 | - |
H-1152 | - |
Homo sapiens | |
0.02 | - |
VX-680 | - |
Homo sapiens | |
0.02 | - |
AG-013736 | - |
Homo sapiens | |
0.02 | - |
CHIR-258 | - |
Homo sapiens | |
0.02 | - |
N-methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-2H-indazol-6-yl}sulfanyl)benzenecarboximidic acid | - |
Homo sapiens | |
0.03 | - |
BAY 439006 | - |
Homo sapiens |