Nek2 Kinase
Nek2 (EC 2.7.11.1), also known as Never in Mitosis (NIMA) related kinase 2, is a 48 kDa homodimeric serine/threonine kinase that is regulated by the cell cycle and is involved in separation of the centrosomes at the start of mitosis.
Nek2 Kinase Inhibitors |
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|---|---|
| Cat. No. | Product Name / Activity |
| 4546 | rac-CCT 250863 |
| Potent Nek2 inhibitor | |
| 4322 | JH 295 |
| Irreversible Nek2 inhibitor | |
| 5150 | NCL 00017509 |
| Potent and reversible NIMA related kinase 2 (Nek2) inhibitor | |
Nek2 (EC 2.7.11.1), also known as Never in Mitosis (NIMA) related kinase 2, is a 48 kDa homodimeric serine/threonine kinase that is regulated by the cell cycle. Nek2 is involved in separation of the centrosomes at the start of mitosis, which ensures proper chromosome separation upon cell division.
Nek2 is localized to the centrosomes and is a member of the Nek family of kinases of which there are eleven members. All Nek kinases have an N-terminal kinase domain and a C-terminal domain containing several regulatory motifs. The regulatory domain differs in size between Nek kinases allowing them to perform different roles within the cell cycle. At least three Nek2 variants exist, Nek2A, Nek2B and Nek2A-T, which result from alternate gene splicing and differ in the length of their C-terminus.
Nek2A dissolves the links between the two centrioles of the centrosome during the G2 phase of the cell cycle. It does this by phosphorylating rootletin, a filamentous linker between the two centrioles, and C-Nap1, which attaches rootletin to the centriole. Phosphorylation allows centriolar separation and the formation of spindle poles enabling correct chromosome separation during mitosis.
Nek2 is overexpressed in numerous cancers, which commonly have an abnormal number of chromosomes, and is associated with cell survival and drug resistance. Inhibition of Nek2 reduces cell growth and increases susceptibility to chemotherapeutic treatments and so Nek2 is of interest in cancer research.
External sources of pharmacological information for Nek2 Kinase :
Literature for Nek2 Kinase
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.
Cancer Metabolism Poster
This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Our Angiogenesis in Cancer poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.
Request copyDownload PDFTaken from the Cancer Product Guide Edition 3
Our Cancer Metabolism poster summarizes the main metabolic pathways in cancer cells, and highlights potential targets for cancer therapeutics.
Request copyDownload PDF
Our Cell Cycle & DNA Damage Repair poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
Request copyDownload PDFTaken from the Cancer Product Guide Edition 3
Our Epigenetics in Cancer poster summarizes the main epigenetic targets in cancer, and highlights chemical compounds for the inhibition of these targets.
Request copyDownload PDF