Tyrosine Kinase Assay Kits

Tyrosine kinases are divided into two main families: the receptor tyrosine kinase (RTK) and cytoplasmic protein (Non-receptor tyrosine kinase). Receptor tyrosine kinases (RTKs) are the high-affinity cell surface receptors for many growth factors, cytokines, and hormones. Both families play critical roles in a variety of cellular signal transduction pathways, regulating such diverse processes as cell division, adhesion, angiogenesis, and survival. These pathways also have a main role in the development and progression of many types of cancer.

• Met
• Pyk2
• FGFR2
• c-Src
• p56Lck
• TrkA
• EphA2
• Wee1

Met Kinase Assay/Inhibitor Screening Kit

CycLex Met Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of recombinant catalytic domain of Met for the rapid and sensitive evaluation of inhibitors or activators.

Met is involved in malignant cell transformation. Increased Met expression has been found in a significant percentage of human cancers and is amplified during the transition between primary tumors and metastasis. Dysregulation of Met activity in cells is thought to be a key event underlying tumor metastasis, and indeed, Met overexpression and hyper activation are reported to correlate with metastatic ability of the tumor cells.

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Pyk2 Kinase Assay/Inhibitor Screening Kit

CycLex Pyk2 Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of recombinant catalytic domain of Pyk2 (Proline-rich Tyrosine Kinase 2) for the rapid and sensitive evaluation of inhibitors or activators.

The focal adhesion PTK family consists of the focal adhesion kinase (FAK) and the Pyk2 kinase (also known as RAFTK, CAK-beta and CADTK). Pyk2 kinase can be activated in response to various stimuli, such as TNF-alpha, changes in osmolality, elevation in intracellular calcium concentration, lysophosphatidic acid, or the addition of bradykinin, a neuropeptide hormone that binds to a G protein-coupled receptor and in turn stimulates phosphatidylinositol hydrolysis.

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FGFR2 Kinase Assay/Inhibitor Screening Kit

CycLex FGFR2 Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of the recombinant catalytic domain of FGFR2 (Fibroblast Growth Factor Receptor 2).

Overexpression and amplification of growth factor receptors are common alterations observed in human breast cancer cells. The FGFR1 and FGFR2 genes are expressed in both normal and breast cancer tissues, and alterations, including amplification and overexpression of FGFR1 and FGFR2, have previously been reported in 5–10% of primary breast cancer specimens. On the other hand, it has been demonstrated that mutations in FGFR2 gene were found in patients with Crouzon syndrome, Apert syndrome, Pfeiffer syndrome, and Jackson-Weiss syndrome.

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c-Src Kinase Assay/Inhibitor Screening Kit

CycLex c-Src Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of recombinant catalytic domain of c-Src for the rapid and sensitive evaluation of inhibitors or activators.

The Src family of non-receptor protein tyrosine kinases play critical roles in a variety of cellular signal transduction pathways, regulating such diverse processes as cell division, motility, adhesion, angiogenesis, and survival. Constitutively activated variants of Src family kinases, including the viral oncoproteins v-Src and v-Yes, are capable of inducing malignant transformation of a variety of cell types. Src family kinases, most notably Src, are frequently overexpressed and/or aberrantly activated in a variety of epithelial and non-epithelial cancers.

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p56Lck Kinase Assay/Inhibitor Screening Kit

CycLex p56Lck Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of recombinant catalytic domain of Lck for the rapid and sensitive evaluation of inhibitors or activators.

Lck is a 56-kDa protein tyrosine kinase that is predominantly expressed in T lymphocytes. A member of the Src kinase family, it has a unique N-terminal region followed by SH3, SH2, and catalytic domains. Lck is an important protein tyrosine kinase in lymphocytes. Its overexpression renders T cells hypersensitive to antigen stimulation, and an Lck-deficient T cell line exhibits dramatically reduced protein tyrosine phosphorylation following T cell receptor (TCR) cross-linking.

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TrkA Kinase Assay/Inhibitor Screening Kit

CycLex TrkA Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of recombinant catalytic domain of TrkA for the rapid and sensitive evaluation of inhibitors or activators.

The Trk (tropomyosin receptor kinase) receptors belong to the family of receptor tyrosine kinases, and three trk genes that have been identified in mammals. The TrkA protooncogene was first identified as a nerve growth factor receptor (NGFR), followed by TrkB and TrkC. Nerve growth factor (NGF) is the preferred ligand for TrkA, brain-derived neurotrophic factor (BDNF) and Neurotrophin-4/5 (NT-4/5) are preferred for TrkB, and Neurotrophin-3 (NT-3) for TrkC. These specificities are not absolute, and NT-3 is also a ligand for TrkA and TrkB.

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EphA2 Kinase Asay/Inhibitor Screening Kit

CycLex EphA2 Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of recombinant catalytic domain of EphA2 for the rapid and sensitive evaluation of inhibitors or activators.

The EphA2 receptor tyrosine kinase belongs to the Eph receptor family. The Eph family contains at least 14 members that are type I transmembrane glycoproteins. Upon cell-cell contact, Eph receptors interact with their ligands called ephrins. EphA2 overexpression correlates with malignant transformation, poor prognosis, metastatic progression, and p53-mediated apoptosis. EphA2 has been detected in tumor neovasculature and was demonstrated to play a role in tumor angiogenesis.

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Wee1 Kinase Assay/Inhibitor Screening Kit

CycLex Wee1 Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of purified Wee1 for the rapid and sensitive evaluation of inhibitors or activators.

The kinases, Wee1 and Chk1 are key regulators of this G2 checkpoint, which act directly or indirectly to inhibit Cdc2 activity. Inhibition of Wee1 and Chk1 sensitized only cancer cells, which lost G1 phase checkpoint, to DNA damage agents-induced apoptosis. These data support the attractiveness of Wee1 as well as Chk1 as molecular targets for abrogating the G2 DNA damage checkpoint arrest, a situation that may selectively sensitize p53-deficient tumor cells to radiation or chemotherapy treatment.

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