 |
|
 |
 |
 |
New Full Length Protein Kinase Substrates
 | | | Protein kinases catalyze the transfer of a phosphate group from ATP to serine, threonine, or tyrosine side chains on their target proteins. Due to their involvement in diseases such as cancer and inflammation, they are the subjects of intense drug discovery research. Traditionally, this research has focused on the development of small molecule inhibitors targeting the catalytic site of the kinase. More recently, however, inhibitors targeting other, allosteric, sites have been sought after. Allosteric inhibitors may target conformational states only present when the kinase binds to its endogenous, protein substrate. For this reason, full length substrates, instead of peptides, are suggested for kinase screens1. Now, you can obtain more biologically relevant results using Calbiochem® Full Length Protein Kinase Substrates. Use the table below to determine which substrate will meet your needs. Obtain consistent kinase screening results by using Calbiochem® Protein Kinase Assay Kits, Inhibitors, and Enzymes.
| | | | | | | Ribbon diagram of c-jun N-terminal kinase (JNK) bound to a peptide inhibitor derived from JNK-interacting protein-1 (J1P1)2. This inhibitor binds outside the ATP-binding site and is thus a non-ATP competitive, or allosteric inhibitor. Development of allosteric inhibitors has prompted the need to use full length protein substrates for protein kinase screening, because some inhibitor binding sites may be present only when a protein kinase interacts with its native substrate. | | | Cat. No. | Product Name | Phosphorylation Sites (Kinase) | | g-Enolase, His?Tag® fusion | Tyr43 (Src); Tyr56, Tyr199, Tyr269 (InsR); Tyr235, Tyr406 (EGFR); Ser39 (cdc2); Thr71, Thr190, Thr320 (PKC); Ser431 (PKA) | | Calmodulin, His?Tag® fusion | Thr44 (CaMK4) | | Casein-a, His?Tag® fusion | Ser71 (PKA); Ser89 (CK-2); Tyr109 (EGFR). | | IRSp53, His?Tag® fusion | Tyr337/Tyr505 (InsR); Tyr471 (Src, EGFR) | | Lipocortin-I, His?Tag® fusion | Tyr20 (EGFR, Abl, Src); Thr215 (PKA); Thr23, Ser26 (PKC) | | Lipocortin-II, His?Tag® fusion | Tyr23 (Src); Ser25 (PKC) | | Myosin Regulatory Light Chain-2, His?Tag® fusion | Ser18 (smMLCK, ROCK1, DLK, ILK) | | PI3K NT-frag., His?Tag® fusion | Ser251 (cdc); Tyr68 (EGFR); Tyr186 (Src); Tyr397 (InsR); Several other Ser/Thr/Tyr sites (CaMII, CKI, CKII, GSK3, PKA, PKG, others) | | Phospholipase C-g-1, His?Tag® fusion | Tyr771, Tyr1253 (EGFR); Tyr783 (Syk); Ser1248 (PKC-a); Tyr432, Tyr775 (FGFR, putative) | | Phospholipase C-g-2, His?Tag® fusion | Tyr753, Tyr759 (Btk, Src, Fyn,Lck); Tyr1217, Tyr1245 (Bcr-Abl) | | Tubulin-a-1, His?Tag® fusion | Tyr172, Tyr210, Tyr224, Tyr282 (EGFR); Tyr440 (InsR) | | Tubulin-g-1, His?Tag® fusion | Tyr92 (InsR); Tyr435, Tyr443 (Src); Thr191, Thr241, Thr443 (PKC) |
| | | | | Related Products | | Protein Kinase Assay Kits | | Inhibitors | | Enzymes | | | | | References 1. Copeland, R. A. 2003. Anal. Biochem. 320, 1. 2. Heo, Y.-S. et al. 2004. EMBO J. 23, 2185. | | |
 |
 |
|
|