Serine/Threonine Kinase Assay Kits

• Rho-kinase
• cGK
• AMPK
• MAPKAP-kinase 2
• Pim-1
• AKT/PKB
• CK2
• CaM-kinase II
• Mps1/TTK
• p38 MAPK
• DYRK2
• Polo-like kinase 1
• Polo-like kinase 3

AMPK Kinase Assay Kit

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).

Related Products

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.

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.

Related Products

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.

Related Products

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.

Related Products

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.

Related Products

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.

Related Products

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.

Related Products

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.

Related Products

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.

Related Products

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.

Related Products

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.

Related Products

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.

Related Products

Product Categories