Table 1.
Characteristics of currently available TAOK inhibitors.
| Compound Name | IUPAC Name | Cell-Based Inhibition Assay (IC50) (Assay Methodology) * | Kinase Inhibition Assay (IC50) (Assay Methodology) * | Reference |
|---|---|---|---|---|
| Compound 43 | N-[2-oxo-2-(1,2,3,4-tetrahydro-naphthalen-1-ylamino)ethyl]biphenyl-4-carboxamide | NA/showed growth inhibition to SK-BR-3 but not MCF-10A cells | TAOK1: 11 ± 0.44 nmol/L (MBPp) TAOK2: 15 ± 1.63 nmol/L (MBPp) Selectively inhibits TAOK1, 2, 3 while showing low inhibition for other 19 kinases |
[33] |
| Compound 63 | N-{3-[(2-{[6-methoxy-1,3-benzothiazol-2yl]amino}-2-oxoethyl)amino]-3-oxo-1-phenylpropyl}benzamide | NA | TAOK1: 19 ± 1.87 nmol/L (MBPp) TAOK2: 39 ± 6.43 nmol/L (MBPp) Selectively inhibits TAOK1, 2, 3 while showing low inhibition for other 19 kinases |
[33] |
| NCGC00188382 | N-[5-[(3,3-dimethylbutan-2-ylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide | 25 to 300 nmol/L in 24 pancreatic cancer cell lines (FA6 cell: ~25 nmol/L; MDA-Panc-28: ~300 nmol/L) (Cytotoxicity assay) | NA/ showed inhibition to the activity of TAOK3, aurora B kinase, and cyclin-dependent kinase 7 in pancreatic cancer cells | [57] |
| SW034538 | N-(2-((2,5-dimethoxyphenyl)amino)-4’-methyl-[4,5’-bithiazol]-2’-yl)propionamide | NA | TAOK2: 300 nmol/L (MBPp) | [84] |
| SW083688 | N-((2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methyl)-3-(3-ethoxypropyl)-4-oxo-2-thioxo-1,2,3,4-tetrahydroquinazoline-7-carboxamide | NA | TAOK2: 1.3 μmol/L (MBPp) | [84] |
* Abbreviations: MBPp: inhibition assay of myelin basic protein phosphorylation; NA: not available.