Haspin

Haspin (histone H3 associated protein kinase), EC 2.7.11.1, is a serine/threonine kinase that has a critical function in mitosis. The enzyme phosphorylates threonine-3 on histone H3 during mitosis.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
5326 CHR 6494 trifluoroacetate
Potent and selective haspin inhibitor
4828 LDN 209929 dihydrochloride
Potent and selective haspin inhibitor

Related Targets

Haspin (histone H3 associated protein kinase), EC 2.7.11.1, is a serine/threonine kinase that has a critical function in mitosis. The enzyme is localized to chromosomes and phosphorylates threonine-3 on histone H3 during mitosis. Phosphorylation of T3 opens up a binding site for the chromosomal passenger complex and activates Aurora B kinase at the centromere. This enables proper chromatid cohesion and metaphase alignment, ensuring normal progression through the cell cycle.

Haspin is a constitutively active enzyme. Studies have shown that during interphase haspin is autoinhibited by a conserved segment of basic residues (haspin basic inhibitory segment or HBIS) within the N-terminal domain, immediately upstream from the kinase domain. The enzyme is reactivated in M phase by Cdk1 phosphorylation of the N-terminus. Phosphorylation leads to recruitment of Polo-like kinase-1 (PLK-1), which further phosphorylates the N-terminal domain of haspin. In addition, the localization of Aurora B kinase to the centromere creates a positive feedback loop that further increases haspin activity.

Haspin is highly expressed in proliferating cells, so is a potential target for cancer therapy. Inhibition of the enzyme has been shown to suppress proliferation of cancer cells both in vitro and in vivo. Haspin is also of interest in spermatogenesis as it is highly expressed in testes.

External sources of pharmacological information for Haspin :

    Literature for Haspin

    Kinases

    Kinases Product Listing

    A collection of over 400 products for kinase research, the listing includes inhibitors of:

    • Receptor Tyrosine Kinases
    • Protein Kinases A, C, D and G
    • PI-3 Kinase, Akt and mTOR
    • MAPK Signaling
    • Receptor Serine/Threonine Kinases
    Cell Cycle & DNA Damage Repair

    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. Adapted from the 2015 Cancer Product Guide, Edition 3, 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.

    Haspin Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    Germ cell associated 2 (haspin) Human GSG2 NM_031965 Q8TF76
    Mouse Gsg2 NM_010353 Q9Z0R0
    Rat Gsg2 XM_001080273 XP_001080273