ProfilerPro Kinase Selectivity Assay Kit 2
Overview
ProfilerPro™ Kinase Selectivity Assay Kit 2 contains all necessary reagents and controls to carry out the rapid in-house screening and profiling of 24 protein kinases against up to 12 different compounds. Enzymes and fluorophore labeled peptide substrates are pre-dispensed into reaction-ready 384 well microtiter plates. Each kinase assay profiling kit will yield a predictable conversion of substrate (non-phosphopeptide) to product (phosphopeptide) at apparent ATP Km. Controls arrayed on the plate enable calculation of percent kinase inhibition of up to 12 customer selected compounds. ProfilerPro™ Kinase Selectivity Assay Kits are read using the Lab-on-a-Chip mobility shift assay technology and the EZ Reader, EZ Reader II or other ProfilerPro compliant reader.
Kit Components:
| Component | Storage Temp |
| Enzyme Plate | -80°C |
| Substrate/ATP Plate | -80°C |
| Reconstitution Buffer | 4°C |
| DDT | -80°C |
| Protease Inhibitor Cocktail | -80°C |
| Termination Buffer | 4°C |
Kinases in ProfilerPro Assay Kit 2
| AMPKa1 | KDR |
| BTK | MARK1 |
| CaMK2d | MST2 |
| CaMK4 | P70S6K |
| CDK2 | PAK2 |
| c-TAK1 | PIM2 |
| DYRK1a | PKCb2 |
| FGFR1 | PKG1a |
| FLT3 | Raf-1 |
| HGK | ROCK2 |
| IGF1R | SGK |
| IRAK4 | SYK |
Applications
Kinase Selectivity Profiling: 96 Kinases, 12 Compounds, 2 Plates
Kinase selectivity profiling is a mainstay of modern drug discovery as target selectivity and specificity are common problems in the identification and development of candidate serine-threonine and tyrosine kinase inhibitors. To adequately assess kinase selectivity and specificity, substantial resources are devoted either to the development and maintenance of in-house kinase profiling panels or to the outsourcing of kinase profiling services. Caliper Life Sciences has developed a kinase profiling system that enables the rapid determination of kinase selectivity against a readily available “off-the-shelf” panel of 96 pharmacologically relevant protein kinases arrayed in ProfilerPro Kinase Selectivity Assay Kits in less than four hours, at the laboratory bench.
The 96 kinases available in the ProfilerPro Kinase Selectivity Assay System were selected due to their therapeutic relevance and diversity across the human kinome. All kinase families are represented in the ProfilerPro Kinase Selectivity Assay System. A complete list of all of the enzymes in the panel is provided in the table above. The human kinome image was reproduced with the permission of Cell Signaling Technology, Inc and first published by Manning G., et al. Science. 2002 Dec 6;298(5600):1912-34.
Kinase selectivity profiling is a mainstay of modern drug discovery as target selectivity and specificity are common problems in the identification and development of candidate serine-threonine and tyrosine kinase inhibitors. To adequately assess kinase selectivity and specificity, substantial resources are devoted either to the development and maintenance of in-house kinase profiling panels or to the outsourcing of kinase profiling services. Caliper Life Sciences has developed a kinase profiling system that enables the rapid determination of kinase selectivity against a readily available “off-the-shelf” panel of 96 pharmacologically relevant protein kinases arrayed in ProfilerPro Kinase Selectivity Assay Kits in less than four hours, at the laboratory bench.
The 96 kinases available in the ProfilerPro Kinase Selectivity Assay System were selected due to their therapeutic relevance and diversity across the human kinome. All kinase families are represented in the ProfilerPro Kinase Selectivity Assay System. A complete list of all of the enzymes in the panel is provided in the table above. The human kinome image was reproduced with the permission of Cell Signaling Technology, Inc and first published by Manning G., et al. Science. 2002 Dec 6;298(5600):1912-34.
Features
ProfilerPro, Expertly Packaged Biochemistry.
The ProfilerPro Kinase Selectivity Assay Panel consists of 96 kinase assays pre-dispensed into reaction ready plates. Just pre-incubate your compounds with the enzymes in the kit, add the matched peptide substrates and ATP (at Km apparent) buffer cocktail and incubate. All enzymes are guaranteed active and configured in reaction ready plates such that the activity of each enzyme will be within its linear range upon detection every time.LabChip Technology, Simply Better Data.
ProfilerPro Kinase Selectivity Assays use LabChip mobility shift detection technology, the only kinase profiling technology that permits the quantification of both substrate (non-phosphorylated peptide) and product (phosphorylated peptide) and the calculation of % conversion directly and without ancillary reagents like antibodies, chelating beads, radioactivity or additional detection steps. Reactants from a kinase assay are sipped from the ProfilerPro kinase assay plate and introduced into a microfluidic chip that does an electrophoretic separation of substrate, product and any compounds that could potentially interfere with other detection technologies.Validation
Kinases Available in ProfilerPro™ Kinase Selectivity Assay Kits
| ProfilerPro Kit 1 | ProfilerPro Kit 2 (P/N 760374) |
| ABL | AMPKa1 |
| AKT1 | BTK |
| AKT2 | CAMK2d |
| AurA | CaMK4 |
| CHK1 | CDK2 |
| CHK2 | c-TAK1 |
| CK1 | DYRK1a |
| Erk1 | FGFR1 |
| Erk2 | FLT3 |
| FYN | HGK |
| GSK3ß | IGF1R |
| INSR | IRAK4 |
| LCK | KDR |
| LYNa | MARK1 |
| MAPKAPK2 | MST2 |
| MAPKAPK5 | P70S6K |
| MET | PAK2 |
| MSK1 | PIM2 |
| p38 | PKCß2 |
| PKAC | PKG1a |
| PKC | Raf-1 |
| PKD2 | ROCK2 |
| RSK1 | SGK |
| SRC | SYK |
24 kinases are available in ProfilerPro™ Kinase Selectivity Assay Kit 2 (P/N 760374).
