Serine/Threonine Kinase Assay Kits

drug discovery

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Aurora-A Aurora Family Kinases AMPK
Rho-kinase  cGK  Checkpoint Kinases
MAPKAP-kinase 2  Pim-1  AKT/PKB 
CK2  CaM-kinase II  PKC Super Family 
p38 MAPK  IKK α and β Mps1/TTK 
PDK1  DYRK2  Polo-like kinase 1 
Polo-like kinase 2  Polo-like kinase 3   

Aurora-A Kinase Assay/Inhibitor Screening Kit

CycLex Aurora-A kinase Assay/Inhibitor Screening Kit is designed to measure the activities of purified Aurora-A for the rapid and sensitive evaluation of inhibitors or activators.

Aurora-A kinase has been shown to contribute to oncogenic transformation and is frequently overexpressed and amplified in many human tumor types. It has been reported that amplification of Aurora-A is present in approximately 12% of primary breast tumors, as well as in breast, ovarian, colon, prostate, neuroblastoma, and cervical cancer cell lines.

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Product Product Code Number
CycLex® Aurora-A Kinase Assay/Inhibitor Screening Kit CY-1165

Aurora Family Kinase Assay/Inhibitor Screening Kit

CycLex Aurora Family Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of purified Aurora family kinases, Aurora A, B, and C kinase for the rapid and sensitive evaluation of inhibitors or activators.

Three distinct Aurora family members, termed Aurora A, B, and C have been described in metazoan organisms. Significant interest in the subject was generated since all three Aurora kinases family members were reported to be overexpressed in many human cancers, and elevated expression has been correlated with chromosomal instability and clinically aggressive disease in some instances.

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CycLex® Aurora Family Kinase Assay/Inhibitor Screening Kit CY-1174

AMPK Kinase Assay Kit 

drug discovery

 

CycLex AMPK Kinase Assay Kit is designed to measure the activities of purified AMP-activated protein kinase (AMPK) or recombinant AMPK.

AMPK regulates cellular energy metabolism by phosphorylation of key enzymes in metabolic pathways, such as acetyl–coenzyme A carboxylase (ACC) or mammalian target of rapamycin (mTOR). Adiponectin and leptin as well as hypoglycaemic drugs are activators of adipose tissue AMPK. This activation probably involves changes in the AMP/ATP ratio, and the upstream kinase LKB1. These results have led to the concept that AMPK has interesting pharmaceutical potential in instances of insulin resistance (type 2 diabetes).

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Product Product Code Number
CycLex® AMPK Kinase Assay Kit      CY-1182
CycLex® AMPKα1 Immunocapture Kinase Assay Kit CY-1186
CycLex® Phospho-AMPKα1 Thr183 ELISA Kit CY-7052

tetramer

Rho-kinase Assay Kit

CycLex Rho-kinase Assay Kit is primarily designed to measure the activities of purified Rho-kinase and DMPK family kinases for the rapid and sensitive evaluation of inhibitors or activators.

Rao et al. (2001) investigated the role of Rho-kinase in the modulation of aqueous humor outflow facility. The treatment of human trabecular meshwork and canal of Schlemm cells with a Rho-kinase-specific inhibitor led to significant but reversible changes in cell shape and decreased actin stress fibers, focal adhesions, and protein phosphotyrosine staining. They suggested Rho-kinase as a potential target for the development of drugs to modulate intraocular pressure in glaucoma patients.

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Product  Product Code Number
CycLex® Rho-kinase Assay Kit CY-1160

Cyclic GMP dependent protein kinase (cGK) Assay Kit

CycLex Cyclic GMP Dependent Protein Kinase (cGK) Assay Kit is designed to measure the activities of purified for the rapid and sensitive evaluation of inhibitors or activators.

Activation of cGK is an important event in the regulation of blood pressure and platelet function. Upstream signals include the generation of nitric oxide (NO) by NO synthases and the subsequent rise in cGMP levels mediated by NO-dependent guanylate cyclases (GCs). The identification of new cGK activators by high throughput screening may lead to the development of a novel class of therapeutics for the treatment of cardiovascular diseases.

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Product Product Code Number
CycLex® Cyclic GMP dependent protein kinase (cGK) Assay Kit CY-1161

Checkpoint Kinase Assay/Inhibitor Screening Kit

CycLex Checkpoint Kinase Assay/Inhibitor Screening Kit-1 is designed to measure the activities of purified checkpoint kinase enzymes such as Chk1, Chk2 and C-TAK1 for the rapid and sensitive evaluation of checkpoint kinase inhibitors using recombinant checkpoint kinases. The phospho-specific monoclonal antibody used in this assay kit has been demonstrated to recognize the phospho-serine 216 residue in Cdc25C, which is phosphorylated by checkpoint kinases.

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Product Product Code Number
CycLex® Checkpoint Kinase Assay/Inhibitor Screening Kit   CY-1162

MAPKAP-kinase 2 Assay/Inhibitor Screening Kit

CycLex MAPKAP-kinase 2 Assay/Inhibitor Screening Kit is designed to measure the activities of purified MAPKAP-kinase 2 for the rapid and sensitive evaluation of inhibitors or activators.

Treatment of cells with endotoxin, interleukin-1, tumor necrosis factor, or various stress stimuli activate p38 MAPK and MAPKAP-kinase 2. MAPKAP-kinase 2 deficient mice showed a reduction in bacterial lipopolysaccharide-induced biosynthesis of tumor necrosis factor (TNF), interferon, IL-1, IL-6, and nitric oxide, suggesting a critical role of MAPKAP-kinase 2 in inflammatory cytokine production.

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Product Product Code Number
CycLex® MAPKAP-kinase 2 Assay/Inhibitor Screening Kit   CY-1166

Pim-1 Kinase Assay/Inhibitor Screening Kit

CycLex Pim-1 Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of purified Pim-1 for the rapid and sensitive evaluation of inhibitors using recombinant Pim-1.

The pim-1 oncogene was originally identified as a genetic locus frequently activated by the proviral insertion of Moloney murine leukemia virus into mouse T cell lymphomas. The pim-1 oncogene has also been implicated in human hematopoietic malignancies, with its overexpression frequently detected in human hematopoietic cell lines as well as in fresh tumor cells from patients with leukemia.

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Product Product Code Number
CycLex® Pim-1 Kinase Assay/Inhibitor Screening Kit CY-1167

AKT/PKB KInase Assay/Inhibitor Screening Kit

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

Mammals have three closely related AKT genes, encoding the isoforms AKT1, AKT2 and AKT3. AKT1 was found to mediate insulin- and insulin-like growth factor (IGF-1)-induced cellular responses, such as the inhibition of glycogen synthase kinase-3, the stimulation of glucose uptake and the promotion of cell survival by inhibiting apoptosis. Overexpression of AKT1 or AKT2 is associated with some human ovarian, pancreatic, and breast carcinomas.

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Product Product Code Number
CycLex® AKT/PKB Kinase Assay/Inhibitor Screening Kit     CY-1168

CK2 (Casein Kinase II) Kinase Assay/Inhibitor Screening Kit

CycLex CK2 Kinase Assay/Inhibitor Screening Kit designed to measure the activities of purified Casein kinase II (CK2) for the rapid and sensitive evaluation of inhibitors or activators. The phospho-serine specific monoclonal antibody used in this assay kit has been demonstrated to recognize the phospho-serine46 residue in p53, which is phosphorylated by CK2 in vitro.

The enzyme is highly expressed in most cancers and this higher expression has been tentatively correlated with the involvement of CK2 in the promotion of specific phases of the cell cycle.

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Product Product Code Number
CycLex® CK2 (Casein Kinase II) Kinase Assay/Inhibitor Screening Kit CY-1170

CaM-kinase II Assay Kit

CycLex CaM kinase II Assay Kit is primarily designed to measure the activities of purified Ca2+/Calmodulin dependent protein kinase II (CaM kinase II) for the rapid and sensitive evaluation of inhibitors or activators.

CaM kinase II is a ubiquitously expressed protein kinase that transduces elevated Ca2+ signals in cells to a number of target proteins ranging from ion channels to transcriptional activators. CaM kinase II has a unique holoenzyme structure and auto regulatory properties that allow it to give a prolonged response to transient Ca2+ signals and to sense cellular Ca2+ oscillations.

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Product Product Code Number
CycLex® CaM-kinase II Assay Kit CY-1173

PKC Super Family Kinase Assay Kit

CycLex PKC Super Family Kinase Assay Kit is primarily designed to measure the activities of purified Protein kinase C (PKC) for the rapid and sensitive evaluation of inhibitors or activators.

Members of PKC family of serine/threonine protein kinases have been implicated in numerous cellular responses in a large variety of cell types. PKC isoenzymes are involved in multiple biochemical processes relevant to cell growth, differentiation, transformation, and play critical roles in transducing signals from a plethora of extracellular receptors, including those for hormones, neurotransmitters, growth factors, and antigens.

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Product Product Code Number
CycLex® PKC Super Family Kinase Assay Kit CY-1175

p38 Kinase Assay/Inhibitor Screening Kit

CycLex p38 Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of purified p38 for the rapid and sensitive evaluation of inhibitors using recombinant p38.

Five homologues/isoforms of p38 MAPK have been identified: p38α, p38β, p38γ, p38δ and p38-2. The p38αMAPK pathway is crucial to inflammatory cytokine production and signaling. Several p38 MAPK inhibitors have been shown to block the production of interleukin-1, tumor necrosis factor and other cytokines. The inhibition of cytokine production seems to result from combined effects at the level of transcription and translation.

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Product Product Code Number
CycLex® p38 Kinase Assay/Inhibitor Screening Kit   CY-1177

IKK α and β Kinase Assay/Inhibitor Screening Kit

CycLex IKK α and β Assay/Inhibitor Screening Kit is designed to measure the activities of purified IKKα and IKKβ for the rapid and sensitive evaluation of inhibitors or activators.

IKK is a multi-subunit complex that contains two catalytic subunits, IKKα and IKKβ, and the regulatory subunit IKKγ. Gene knockout studies have clearly demonstrated that IKKβ and IKKγ subunits of the IKK complex are required for NF-κB activation by all known pro-inflammatory stimuli including lipopolysaccharide (LPS), TNF, and IL-1. Thus, a selective inhibitor of IKKβ would not only be of great interest as a potential anti-inflammatory agent but also as a valuable tool to understand the mechanisms regulating NF-κB activation by these inflammatory agonists.

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Product Product Code Number
CycLex® IKKα and β Kinase Assay/Inhibitor Screening Kit   CY-1178

Human Mps1/TTK Kinase Assay/Inhibitor Screening Kit 

CycLex Human Mps1/TTK Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of purified human Mps1/TTK for the rapid and sensitive evaluation of inhibitors or activators.

Human Mps1 is detectable in all proliferating human cells and tissues. When cells are induced to enter the cell cycle, levels of human Mps1 mRNA, protein and kinase activity increase at the G1/S phase of the cell cycle and peak in G2/M. Human Mps1 mRNA levels, as well as kinase activity, drop sharply in early G1, whereas protein levels are largely maintained. Human Mps1 may play a role in cell cycle control.

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Product Product Code Number
CycLex® Mps1/TTK Kinase Assay/Inhibitor Screening Kit   CY-1179

PDK1 Kinase Assay/Inhibitor Screening Kit

CycLex PDK1 Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of purified PDK1. PDK1 (3-phosphoinositide dependent protein kinase-1) plays an important role in insulin and growth factor signaling cascades. It is known to phosphorylate and activate at least 24 protein kinases that comprise the Akt /PKB. It has been reported that high level of activated Akt is present in a large percentage (30–60%) of common tumor types, including melanoma and breast, lung, gastric, prostate, hematological, and ovarian cancers. The PDK1/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor angiogenesis and thus represents an attractive target for the development of small molecule inhibitors that may be useful in the treatment of cancer.

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Product Product Code Number
CycLex® PDK1 Kinase Assay/Inhibitor Screening Kit   CY-1180

DYRK2 Kinase Assay/Inhibitor Screening Kit

CycLex DYRK2 Kinase Assay/Inhibitor Screening Kit is designed to measure the activities of purified DYRK2 for the rapid and sensitive evaluation of inhibitors or activators.

It was reported that DYRK2 was overexpressed in both lung and esophageal adenocarcinomas showing gene amplification at 12q14. Recently Taira et al. reported that in response to genotoxic stress, DYRK2 translocated into the nucleus and phosphorylated p53 on ser46, inducing P53AIP1 expression and apoptosis in a ser46 phosphorylation-dependent manner. These results suggest that DYRK2 regulates p53 to induce apoptosis in response to DNA damage.

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Product Product Code Number
CycLex® DYRK2 Kinase Assay/Inhibitor Screening Kit   CY-1181

Polo-like kinase 1 Assay/Inhibitor Screening Kit

CycLex Polo-like kinase 1 Assay/Inhibitor Screening Kit is designed to measure the activities of purified polo-like kinase 1 (Plk1) for the rapid and sensitive evaluation of inhibitors using recombinant Plk1.

Elevated expression of Plk1 occurs in many different types of cancer, and Plk1 has been proposed as a diagnostic marker for several tumors. Liu and Erikson used the vector-based small interfering RNA (siRNA) technique to specifically deplete Plk1 in cancer cells. They found that such depletion dramatically inhibited cell proliferation, decreased viability, and resulted in cell-cycle arrest with a 4n DNA content. The data supported the notion that disruption of Plk1 function could be an important application in cancer therapy.

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Product Product Code Number
CycLex® Polo-like kinase 1 Assay/Inhibitor Screening Kit   CY-1163

Polo-like kinase 2 Assay/Inhibitor Screening Kit

CycLex Polo-like Kinase 2 Assay/Inhibitor Screening Kit is designed to measure the activities of purified Polo-like kinase 2 (Plk2) for the rapid and sensitive evaluation of inhibitors using recombinant Plk2.

Plk2, also called Snk, a member of polo-like kinase family, was originally identified as immediate-to-early transcripts in mouse fibroblasts. It is expressed mainly in the hippocampal neurons in the brains of adult rodents and the precise function of Plk2 is uncertain. However, from analysis of Plk2-/- mice, it appears that the protein has a role in development and is involved in cell-cycle progression. Plk2 protein is expressed at equal abundance during G1, S, and G2 phases in HeLa cell. Plk2 kinase activity peaked as near the G1-to-S transition and decreased again as cells entered G2 phase of the cell cycle.

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Product Product Code Number
CycLex® Polo-like kinase 2 Assay/Inhibitor Screening Kit   CY-1183

Polo-like kinase 3 Assay/Inhibitor Screening Kit

CycLex Polo-like Kinase 3 Assay/Inhibitor Screening Kit is designed to measure the activities of purified Polo-like kinase 3 (Plk3) for the rapid and sensitive evaluation of inhibitors or activators.

The polo-like kinases are a family of conserved serine/threonine kinases that play a critical role in the normal progression of cells through mitosis. The Plk3 serine/threonine kinase is a mammalian member of this family. Plk3 has been suggested as a candidate tumor suppressor, and its expression is down-regulated or absent in lung carcinomas and squamous cell carcinomas of the head and neck.

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Product Product Code Number
CycLex® Polo-like kinase 3 Assay/Inhibitor Screening Kit     CY-1176