Kinases
Protein kinases are a group of enzymes with basic biochemical function of phosphorylation of other proteins. Protein kinase, as a class of proteins, represents one of the most important classes of cellular proteins. As the principle components of cell signal transduction pathways, the activity of kinases often controls the activities of “effector” protein, which in turn affecting the profiles of cellular gene expressions.Kinase signaling pathways play a fundamental role in regulating cell proliferation, cell metabolism and cell death. Research shows that changes in protein kinase activity within a cell can lead to several disease states, most notably cancer. With this knowledge base, scientists have been investigating the ability of drugs to block various protein kinases as a cancer therapy. This approach has proved successful with the discovery of several kinase inhibitor drugs for the treatment of various cancers such as Gleevec®, Iressa® and Tarceva®. In addition to their involvement in cancer, protein kinases are implicated in diabetes, inflammation and neurological development and degeneration.
| Cat# | Assay Type | Assay Class | Assay Name | $/Well (USD) |
|---|---|---|---|---|
| 200-0924 | Enzyme | Lipid | PI3Ka (p110a/p85a) (h) | $25.00 |
| 200-0775 | Enzyme | Lipid | Sphingosine SK1 (h) | $25.00 |
| 200-0776 | Enzyme | Lipid | Sphingosine SK2 (h) | $25.00 |
| 200-0832 | Enzyme | Protein | Abl (E255K) (h) | $25.00 |
| 200-0833 | Enzyme | Protein | Abl (G250E) (h) | $25.00 |
| 200-0409 | Enzyme | Protein | Abl (h) | $25.00 |
| 200-0834 | Enzyme | Protein | Abl (Q252H) (h) | $25.00 |
| 200-0839 | Enzyme | Protein | Abl (T315I) (h) | $25.00 |
| 200-0410 | Enzyme | Protein | Akt1 (PKBa) (h) | $25.00 |
| 200-0411 | Enzyme | Protein | Akt2 (PKBb) (h) | $25.00 |
| 200-0457 | Enzyme | Protein | Akt3 (PKBg) (h) | $25.00 |
| 200-0823 | Enzyme | Protein | AMPKa1 (h) | $25.00 |
| 200-0412 | Enzyme | Protein | AurA (Aur2/STK6) (h) | $25.00 |
| 200-0812 | Enzyme | Protein | AurB (h) | $25.00 |
| 200-0816 | Enzyme | Protein | AurC (AURKC) (h) | $25.00 |
| 200-0459 | Enzyme | Protein | Axl (h) | $25.00 |
| 200-0920 | Enzyme | Protein | BLK (h) | $25.00 |
| 200-0460 | Enzyme | Protein | BMX (h) | $25.00 |
| 200-0769 | Enzyme | Protein | BTK (h) | $25.00 |
| 200-0418 | Enzyme | Protein | c-Kit (h) | $25.00 |
| 200-0420 | Enzyme | Protein | c-TAK (h) | $25.00 |
| 200-0821 | Enzyme | Protein | CaMK2a (h) | $25.00 |
| 200-0760 | Enzyme | Protein | CaMK2a (rat) | $25.00 |
| 200-0859 | Enzyme | Protein | CAMK2d (h) | $25.00 |
| 200-0770 | Enzyme | Protein | CaMK4 (h) | $25.00 |
| 200-0414 | Enzyme | Protein | CDK2/cyclinA (h) | $25.00 |
| 200-0777 | Enzyme | Protein | CDK6 (h) | $25.00 |
| 200-0840 | Enzyme | Protein | CDK9/cyclin 1 (h) | $25.00 |
| 200-0480 | Enzyme | Protein | CHK1 (CHEK1) (h) | $25.00 |
| 200-0417 | Enzyme | Protein | CHK2 (CHEK2) (h) | $25.00 |
| 200-0778 | Enzyme | Protein | CK1a (CSNK1A1) (h) | $25.00 |
| 200-0461 | Enzyme | Protein | CK1d (CSNK1D) (h) | $25.00 |
| 200-0462 | Enzyme | Protein | CK2a1b (h) | $25.00 |
| 200-0477 | Enzyme | Protein | COT (Tpl2, MAP3K8) | $25.00 |
| 200-0774 | Enzyme | Protein | cRAF (RAF1) (h) | $25.00 |
| 200-0419 | Enzyme | Protein | CSK (h) | $25.00 |
| 200-0815 | Enzyme | Protein | DYRK1a (h) | $25.00 |
| 200-0890 | Enzyme | Protein | DYRK1b (h) | $25.00 |
| 200-0422 | Enzyme | Protein | DYRK2 (h) | $25.00 |
| 200-0463 | Enzyme | Protein | EGFR (ErbB1) (h) | $25.00 |
| 200-0837 | Enzyme | Protein | EGFR (L858R) (h) | $25.00 |
| 200-0836 | Enzyme | Protein | EGFR (L861Q) (h) | $25.00 |
| 200-0835 | Enzyme | Protein | EGFR (T790M) (h) | $25.00 |
| 200-0849 | Enzyme | Protein | EphA1 (h) | $25.00 |
| 200-0771 | Enzyme | Protein | EphA2 (h) | $25.00 |
| 200-0850 | Enzyme | Protein | EphA3 (h) | $25.00 |
| 200-0851 | Enzyme | Protein | EphA4 (h) | $25.00 |
| 200-0852 | Enzyme | Protein | EphA5 (h) | $25.00 |
| 200-0853 | Enzyme | Protein | EphA6 (h) | $25.00 |
| 200-0854 | Enzyme | Protein | EphA7 (h) | $25.00 |
| 200-0856 | Enzyme | Protein | EphA8 (h) | $25.00 |
| 200-0857 | Enzyme | Protein | EphB1 (h) | $25.00 |
| 200-0824 | Enzyme | Protein | EphB2 (h) | $25.00 |
| 200-0858 | Enzyme | Protein | EphB3 (h) | $25.00 |
| 200-0464 | Enzyme | Protein | EphB4 (h) | $25.00 |
| 200-0825 | Enzyme | Protein | ErbB2 (HER2) (h) | $25.00 |
| 200-0347 | Enzyme | Protein | ErbB4 (HER4) (h) | $25.00 |
| 200-0767 | Enzyme | Protein | FAK2 (PYK2/PTK2b) (h) | $25.00 |
| 200-0779 | Enzyme | Protein | FGFR1 (h) | $25.00 |
| 200-0761 | Enzyme | Protein | FGFR3 (h) | $25.00 |
| 200-0802 | Enzyme | Protein | FGFR4 (h) | $25.00 |
| 200-0803 | Enzyme | Protein | Flt1 (VEGFR1) (h) | $25.00 |
| 200-0831 | Enzyme | Protein | Flt3 (D835Y) (h) | $25.00 |
| 200-0423 | Enzyme | Protein | Flt3 (h) | $25.00 |
| 200-0804 | Enzyme | Protein | Flt4 (VEGFR3) (h) | $25.00 |
| 200-0805 | Enzyme | Protein | FMS (CSF1R) (h) | $25.00 |
| 200-0762 | Enzyme | Protein | Fyn (h) | $25.00 |
| 200-0424 | Enzyme | Protein | GSK-3alpha (h) | $25.00 |
| 200-0425 | Enzyme | Protein | GSK-3beta (h) | $25.00 |
| 200-0808 | Enzyme | Protein | HGK (ZC1/MAP4K4) (h) | $25.00 |
| 200-0466 | Enzyme | Protein | IGF1R (h) | $25.00 |
| 200-0780 | Enzyme | Protein | IKKa (h) | $25.00 |
| 200-0772 | Enzyme | Protein | IKKb (h) | $25.00 |
| 200-0467 | Enzyme | Protein | InsR (h) | $25.00 |
| 200-0763 | Enzyme | Protein | IRAK4 (h) | $25.00 |
| 200-0465 | Enzyme | Protein | Jak2 (h) | $25.00 |
| 200-0933 | Enzyme | Protein | Jak3 (h) | $25.00 |
| 200-0773 | Enzyme | Protein | JNK2 (h) | $25.00 |
| 200-0768 | Enzyme | Protein | KDR (VEGFR2, FLK1) (h) | $25.00 |
| 200-0427 | Enzyme | Protein | Lck (h) | $25.00 |
| 200-0842 | Enzyme | Protein | LTK (h) | $25.00 |
| 200-0428 | Enzyme | Protein | LynA (h) | $25.00 |
| 200-0813 | Enzyme | Protein | LynB (h) | $25.00 |
| 200-0747 | Enzyme | Protein | MAPK1 (ERK2, p42mapk) (h) | $25.00 |
| 200-0433 | Enzyme | Protein | MAPK11 (p38beta) (h) | $25.00 |
| 200-0434 | Enzyme | Protein | MAPK12 (p38gamma, SAPK3, ERK6) (h) | $25.00 |
| 200-0435 | Enzyme | Protein | MAPK13 (p38delta, SAPK4) (h) | $25.00 |
| 200-0432 | Enzyme | Protein | MAPK14 (p38alpha, SAPK2alpha) (h) | $25.00 |
| 200-0754 | Enzyme | Protein | MAPK3 (ERK1, p44mapk) (h) | $25.00 |
| 200-0430 | Enzyme | Protein | MAPKAPK2 (h) | $25.00 |
| 200-0441 | Enzyme | Protein | MAPKAPK5 (PRAK) (h) | $25.00 |
| 200-0826 | Enzyme | Protein | MARK1 (h) | $25.00 |
| 200-0855 | Enzyme | Protein | MELK (h) | $25.00 |
| 200-0844 | Enzyme | Protein | Mer (h) | $25.00 |
| 200-0469 | Enzyme | Protein | MET (h) | $25.00 |
| 200-0431 | Enzyme | Protein | MSK1 (RPS6KA5) (h) | $25.00 |
| 200-0429 | Enzyme | Protein | MST2 (STK3) (h) | $25.00 |
| 200-0918 | Enzyme | Protein | MST4 (h) | $25.00 |
| 200-0471 | Enzyme | Protein | NEK2 (h) | $25.00 |
| 200-0436 | Enzyme | Protein | p70S6K (h) | $25.00 |
| 200-0437 | Enzyme | Protein | PAK2 (h) | $25.00 |
| 200-0916 | Enzyme | Protein | PAK4 (h) | $25.00 |
| 200-0838 | Enzyme | Protein | PDGFa (D842V) (h) | $25.00 |
| 200-0438 | Enzyme | Protein | PDGFRa (h) | $25.00 |
| 200-0472 | Enzyme | Protein | PDGFRb (h) | $25.00 |
| 200-0439 | Enzyme | Protein | PDK1 (h) | $25.00 |
| 200-0906 | Enzyme | Protein | Pim1 (h) | $25.00 |
| 200-0473 | Enzyme | Protein | Pim2 (h) | $25.00 |
| 200-0440 | Enzyme | Protein | PKA (h) | $25.00 |
| 200-0334 | Enzyme | Protein | PKC-alpha (h) | $25.00 |
| 200-0335 | Enzyme | Protein | PKC-b1 (PRKCB1) (h) | $25.00 |
| 200-0336 | Enzyme | Protein | PKC-b2 (PRKCB2) (h) | $25.00 |
| 200-0337 | Enzyme | Protein | PKC-d (PRKCD) (h) | $25.00 |
| 200-0346 | Enzyme | Protein | PKC-eta (PRKCH) (h) | $25.00 |
| 200-0338 | Enzyme | Protein | PKC-g (PRKCG) (h) | $25.00 |
| 200-0807 | Enzyme | Protein | PKC-theta (PRKCQ) (h) | $25.00 |
| 200-0765 | Enzyme | Protein | PKC-z (PRKCZ) (h) | $25.00 |
| 200-0748 | Enzyme | Protein | PKD2 (h) | $25.00 |
| 200-0809 | Enzyme | Protein | PKG1a (h) | $25.00 |
| 200-0810 | Enzyme | Protein | PKG1b (h) | $25.00 |
| 200-0766 | Enzyme | Protein | PLK1 (h) | $25.00 |
| 200-0841 | Enzyme | Protein | RET (h) | $25.00 |
| 200-0919 | Enzyme | Protein | ROCK1 (h) | $25.00 |
| 200-0442 | Enzyme | Protein | ROCK2 (h) | $25.00 |
| 200-0475 | Enzyme | Protein | RSK1 (p90RSK/RPS6KA1) (h) | $25.00 |
| 200-0820 | Enzyme | Protein | RSK2 (h) | $25.00 |
| 200-0782 | Enzyme | Protein | RSK3 (h) | $25.00 |
| 200-0476 | Enzyme | Protein | SGK1 (h) | $25.00 |
| 200-0915 | Enzyme | Protein | skMLCK (MYLK2) (h) | $25.00 |
| 200-0443 | Enzyme | Protein | Src (h) | $25.00 |
| 200-0444 | Enzyme | Protein | Syk (h) | $25.00 |
| 200-0827 | Enzyme | Protein | Tie2 (h) | $25.00 |
| 200-0783 | Enzyme | Protein | TrkA (NTRK1) (h) | $25.00 |
| 200-0811 | Enzyme | Protein | TrkB (NTRK2) (h) | $25.00 |
| 200-0819 | Enzyme | Protein | TrkC (NTRK3) (h) | $25.00 |
| 200-0814 | Enzyme | Protein | TTK (h) | $25.00 |
| 200-0843 | Enzyme | Protein | TYRO3 (h) | $25.00 |
| 200-0935 | Enzyme | Protein | YES (h) | $25.00 |
| 200-0479 | Enzyme | Protein | ZAP70 (h) | $25.00 |
CDAS conducts in vitro kinase profiling and high throughput screening services using the LabChip 3000 and EZ Reader microfluidic technology platforms developed by Caliper Life Sciences. This platform does not require monoclonal antibodies or radioisotopes and thus is ideal for detecting biochemical inhibition in a direct, ratiometric, high quality format. As an example, not only can serine/threonine and receptor tyrosine kinases be readily assayed, but also inhibitors of lipid kinases such as PI3 kinase (e.g. PI3K-alpha) and sphingosine kinase are easily detected.
Lead discovery and pharmacology scientists can profile lead compounds through the entire kinase panel, or through a customized set of assays, at either a single concentration or in dose response studies (IC50) to evaluate compound selectivity. Customers can also select a single assay, or a small panel, for profiling large numbers of compounds for lead optimization studies. In addition to outsourced kinase selectivity screening, CDAS also performs contract assay development services for enzyme targets using the LC3000 and EZ platforms.