Mps1

AZ 3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nM). It interferes with chromosome alignment and overrides spindle assembly checkpoint and also Inhibits the recruitment of Mad1, Mad2 and centromere protein E (CENP-E) to kinetochores.

Mps1-IN-1 is a highly potent and selectibe Mpsl inhibitor with IC50 of 367 nM; >1000-fold selectivity relative to the 352 member kinase panel with the major exceptions of Alk and Ltk.

MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1

Luvixasertib hydrochloride is a highly selective inhibitor of TTK/Mps1, demonstrating an IC50 of 1.7 nM for TTK in vitro. This compound exhibits significant anti-cancer activity, making it a valuable tool for cancer research. Its mechanism of action targets crucial mitotic processes, providing insights into cell cycle regulation and tumorigenesis. Luvixasertib hydrochloride is suitable for studies focused on cancer biology and therapeutic development.

CFI-401980 is a selective inhibitor of the MPS1 kinase, exhibiting an affinity characterized by a Ki value of 0.8 nM. This compound effectively inhibits the proliferation of HCT116 cancer cell lines, making it a valuable tool in cancer research. CFI-401980 may be utilized to investigate the role of MPS1 in cell cycle regulation and its potential as a therapeutic target in anti-cancer strategies.

TC-Mps1-12 is a highly selective inhibitor of monopolar spindle 1 (Mps1), demonstrating an IC50 of 6.4 nM. It effectively disrupts the function of Mps1, a key regulator of the mitotic spindle assembly checkpoint. This compound is valuable for studying cell cycle regulation, mitosis, and cancer biology, facilitating research into potential therapeutic targets for cancer treatment.

NTRC 0066-0 is a potent inhibitor of threonine-tyrosine kinase (TTK), exhibiting an IC50 of 0.9 nM. This selective inhibitor is valuable for cancer research, offering insights into TTK-mediated signaling pathways and their role in tumorigenesis. NTRC 0066-0 enables the exploration of TTK's contribution to cell cycle regulation and cancer cell proliferation.

Mps1-IN-7 is a potent inhibitor of MPS1 with an IC50 value of 0.020 μM, demonstrating selectivity over JNK1 and JNK2 (IC50 values of 0.11 μM and 0.22 μM, respectively). This compound exhibits significant antiproliferative effects across various cancer cell lines, including SW620, CAL51, Miapaca-2, and RMG1, with GI50 values of 0.065, 0.068, 0.25, and 0.110 μM, respectively. Mps1-IN-7 can be utilized in research focused on cell cycle regulation and the development of targeted cancer therapies.

RMS-07 is a covalent inhibitor of Monopolar Spindle Kinase 1 (MPS1/TTK), exhibiting an apparent IC50 of 13.1 nM. It selectively targets a poorly conserved cysteine residue within the kinase's hinge region. This compound is utilized in research applications focusing on cell cycle regulation, mitotic checkpoint studies, and cancer therapeutics.

Mps1-IN-3 hydrochloride is a potent and selective inhibitor of Mps1, with an IC50 value of 50 nM. This compound effectively inhibits the proliferation of glioblastoma cells and enhances the sensitivity of glioblastomas to Vincristine in orthotopic glioblastoma xenograft models. Mps1-IN-3 hydrochloride is valuable for research applications targeting cell cycle regulation and glioblastoma treatment strategies.

Mps1-IN-10 is a potent inhibitor of Mps1, exhibiting an IC50 of 6.4 nM. This compound effectively suppresses the proliferation of cancer cells, demonstrated by a GI50 of 11 nM in the MDA-MB-231 cell line. Mps1-IN-10 also shows significant anti-tumor efficacy in preclinical models using MDA-MB-231 xenografts, making it a valuable tool for cancer research applications focused on cell cycle regulation and tumor growth inhibition.

TTK Inhibitor 3 is a highly potent and selective inhibitor of TTK, a critical enzyme involved in the spindle assembly checkpoint. With an IC50 value of 3.0 nM, this compound effectively disrupts TTK activity, making it a valuable tool for studying cell cycle regulation and mitotic progression. Its application extends to research focused on cancer biology, particularly in the context of therapeutic approaches targeting aberrant cell division.

Mps1-IN-1 dihydrochloride is a potent ATP-competitive inhibitor of Mps1 kinase, exhibiting an IC50 of 367 nM. This compound effectively inhibits Mps1 mitotic kinase activity, disrupting spindle assembly checkpoint (SAC) function and leading to compromised cell cycle regulation. Mps1-IN-1 dihydrochloride demonstrates cytotoxic effects in various cellular contexts, impacting both cancerous and normal cells, making it a valuable tool for research in cell division and cancer therapy.

Mps1-IN-6 is a selective inhibitor of Mps1, exhibiting an IC50 value of 2.596 nM. This compound demonstrates significant antiproliferative effects and shows potential as an effective antitumor agent. Mps1-IN-6 is valuable for research into tumor biology and potential therapeutic interventions targeting mitotic checkpoint regulation.

Mps1-IN-4 is a selective inhibitor of Monopolar spindle 1 (Mps1), a critical kinase involved in the regulation of the mitotic checkpoint. This compound exhibits antiproliferative activity, making it a valuable tool for cancer research. Mps1-IN-4 can be utilized to investigate the role of Mps1 in cell cycle regulation and its implications in tumorigenesis.

TTK inhibitor 4 is a potent inhibitor of threonine tyrosine kinase (TTK), exhibiting an IC50 value of 0.016 μM. This compound demonstrates significant anti-tumor activity, making it a valuable tool for cancer research. It is particularly relevant for studies focused on cell proliferation, apoptosis, and signal transduction pathways associated with malignancies.

Mps1-IN-8 is a potent inhibitor of the Mps1 kinase, a key regulator of the spindle assembly checkpoint. It effectively impairs Mps1 activity, leading to mitotic disruption in cancer cells. This compound is valuable for investigating the role of Mps1 in tumorigenesis and exploring its potential as a therapeutic target in cancer research.

CFI-400936 is a potent inhibitor of the TTK protein kinase, demonstrating an IC50 of 3.6 nM. This compound exhibits significant antitumor activity, making it valuable for research focused on cancer treatment and cellular proliferation studies. Its ability to modulate TTK activity positions it as a useful tool for investigating therapeutic strategies in oncology.

ONCOII is a potent Mps1 inhibitor with an IC50 of 10.8 nM, primarily targeting the Mps1 kinase involved in cell division and checkpoint regulation. This reagent's efficacy is influenced by specific mutations in the Mps1 gene, as cells harboring such mutations show increased resistance to ONCOII. It is particularly useful in cancer research to study cell cycle dynamics and the effects of Mps1 modulation in tumorigenesis.

Mps-BAY2b is a potent inhibitor of monopolar spindle 1 (MPS1) with an IC50 of 14 nM in human MPS1. This compound demonstrates significant anticancer activity, making it a valuable tool for cancer research. Mps-BAY2b can be utilized in studies to investigate cell cycle regulation and the mechanisms of tumor progression.

Mps1/TTK-IN-1 is a potent Mps1 kinase inhibitor that specifically binds to the ATP-binding pocket of the enzyme with an IC50 of 9.2 nM and a Kd of 1.6 nM. It effectively inhibits Mps1 activity, including in drug-resistant mutants (C604Y and C604W) with IC50 values of 170 nM and 19 nM, respectively. By blocking the phosphorylation of the kinetochore protein KNL1, Mps1/TTK-IN-1 disrupts spindle assembly checkpoint function and hinders proper chromosome separation, ultimately inhibiting mitosis and tumor cell proliferation, making it a valuable tool for cancer research.