2. Signaling Pathways
  3. Cell Cycle/DNA Damage
    Cytoskeleton
  4. Mps1

Mps1

Monopolar spindle 1

Mps1

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Monopolar spindle 1 (Mps1/TTK) is a serine/threonine kinase conserved from yeast to human. It has been shown to function as the key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughter cells.

MPS1, a dual specificity protein kinase, is also one of the main components of the SAC and ensures cells do not progress from metaphase to anaphase until the kinetochores are properly attached to the microtubules and under the appropriate tension at the metaphase plate. Cancer cells heavily rely on MPS1 to cope with aneuploidy resulting from aberrant numbers of chromosomes. The kinase has been found to be upregulated in a large number of tumor types. Mps1 is an attractive oncology target due to its high expression level in cancer cells as well as the correlation of its expression levels with histological grades of cancers.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-123675
    CFI-400936
    		Inhibitor
    CFI-400936 is a potent TTK inhibitor with an IC50 of 3.6 nM. CFI-400936 has antitumor activity.
    CFI-400936
  • HY-101340AR
    Luvixasertib hydrochloride (Standard)
    		Inhibitor
    Luvixasertib (hydrochloride) (Standard) is the analytical standard of Luvixasertib (hydrochloride) (HY-101340A). This product is intended for research and analytical applications. CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50 of 1.7 nM for TTK in vitro. CFI-402257 hydrochloride has anti-cancer activity.
    Luvixasertib hydrochloride (Standard)
  • HY-164518
    PF-3837
    		Inhibitor
    PF-3837 is an Mps1 kinase inhibitor with a Ki value of 0.33 nM and an IC50 value of 5.5 nM. PF-3837 interferes with the cell cycle checkpoint by inhibiting Mps1 catalytic activity, reducing genomic stability, thereby inducing cancer cell apoptosis (Apoptosis). PF-3837 can be used in research on breast cancer.
    PF-3837
  • HY-164516
    ONCOII
    		Inhibitor
    ONCOII is an Mps1 inhibitor with an IC50 of 10.8 nM. The inhibitory activity of ONCOII against Mps1 is affected by naturally occurring mutations in the Mps1 gene, and cells with Mps1 mutations exhibit increased resistance to ONCOII. ONCOII can be used in cancer research.
    ONCOII
  • HY-120704
    Mps-BAY2b
    		Inhibitor
    Mps-BAY2b is a oral active monopolar spindle 1 (MPS1) inhibitor with the IC50 of 14 nM (human MPS1). Mps-BAY2b shows anticancer activity and can be used for study of cancer.
    Mps-BAY2b
  • HY-116470
    Mps1/TTK-IN-1
    		Inhibitor
    Mps1/TTK-IN-1 (Compound cpd-5), a derivative of NMS-P715 (HY-12382), is a Mps1 kinase inhibitor with an IC50 of 9.2 nM and a Kd of 1.6 nM. Mps1/TTK-IN-1 specifically targets the ATP-binding pocket of the Mps1 kinase. Mps1/TTK-IN-1 maintains inhibitory activity against Mps1 drug-resistant mutants (C604Y, C604W) with IC50 values of 170 and 19 nM and Kd values of 471 and 349 nM. Mps1/TTK-IN-1 can block the phosphorylation of kinetochore protein KNL1 mediated by Mps1, interfere with the spindle assembly checkpoint function, prevent the correct separation of chromosomes, and thereby inhibit the mitosis and proliferation of tumor cells.
    Mps1/TTK-IN-1
  • HY-164519
    PF-7006
    		Inhibitor
    PF-7006 is an Mps1 kinase inhibitor with a Ki value of 0.27 nM and an IC50 value of 2.5 nM. PF-7006 interferes with cell cycle checkpoints by inhibiting the catalytic activity of Mps1, reducing histone H3 levels, and shortening the duration of mitosis, leading to apoptosis in cancer cells. Combined use of PF-7006 with Palbociclib (HY-50767) increases cancer cell tolerance to PF-7006. PF-7006 can be used for breast cancer research.
    PF-7006
Cat. No. Product Name / Synonyms Application Reactivity