Mps1

Mps1-IN-1 is a potent, selective, and ATP-competitive inhibitor of Mps1 kinase (IC50: 367 nM).

Mps1-IN-2 is a potent, selective, and ATP-competitive inhibitor of both Mps1 and Plk1.

BOS-172722 is an inhibitor of the monopolar spindle 1 (MPS1) checkpoint with an IC50 of 2 nM.

CFI-402257 is a selective inhibitor of Mps1 TTK kinase (Mps1 Ki = 0.09 nM; EC50 = 6.5 nM)and can be used in studies about hepatocellular carcinoma diseases.

MPI-0479605 is an ATP competitive and selective inhibitor.

Mps1-IN-3 is an effective and selective inhibitor of MPS1 kinase (IC50: 50 nM).

TC-Mps1-12 is an effective and selective inhibitor of monopolar spindle 1 (IC50: 6.4 nM) .

Mps1-IN-9 (compound M-12) is a targeted Mps1 drug discovered for broad-spectrum antifungal medication use.

PROTAC MPS1 Degrader 2 (Compound 15) is a potent degrader of monopolar spindle 1 (Mps1, TTK), AURKA, and AURKB with DC50 values of 42.0, 2.1, and 154.0 nM respectively. It is utilized in the research of acute myeloid leukemia.

PROTAC MPS1 degrader 1 (Compound 19) acts as a potent degrader of Monopolar spindle 1 (Mps1, TTK), AURKA, and AURKB, with DC50 values of 17.7, 108.7, and 570.3 nM respectively. It is utilized in the study of acute myeloid leukemia. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase)

MPS1/TTK inhibitor is an inhibitor of monopolar spindle 1 (MPS1/TTK; IC50 = 5.8 nM), a kinase involved in mitotic spindle checkpoint signaling that is overexpressed in certain cancerous tumors. It inhibits MPS1 phosphorylation of kinetochore scaffold 1 (KNL1) and increases the rate of mitosis and the number of cells entering anaphase within 15 minutes, indicating MPS1 checkpoint inhibition, when used at a concentration of 100 nM. MPS1/TTK inhibitor (50 and 100 nM) increases the number of missegregated chromosomes, with an increased number of errors at 100 nM compared with 50 nM. It also inhibits colony formation of DLD1, HCT116, and U2OS cells (IC50s = 24.6, 20.1, and 20.6 nM, respectively).

Mps1-IN-3 hydrochloride is a potent and selective inhibitor of Mps1 (IC50: 50 nM) that exhibits inhibitory effects on the proliferation of glioblastoma cells and effectively sensitizes glioblastomas to vincristine in an in situ xenograft tumor model.

Mps1-IN-1 dihydrochloride, a potent ATP-competitive inhibitor of Mps1 kinase, exhibits an IC50 of 367 nM. It effectively inhibits the activity of Mps1 mitotic kinase and disrupts spindle assembly checkpoint (SAC) function, thereby reducing the viability of both cancerous and 'normal' cells.

Mps1-IN-4 is a compound that selectively inhibits Monopolar spindle 1 (Mps1), exhibiting antiproliferative properties useful in cancer research.

Mps1-IN-5 is a potent, orally active Mps1 inhibitor exhibiting an IC50 of 29 nM, known for triggering apoptosis and G2 M phase cell cycle arrest. This compound demonstrates antiproliferative and anti-tumor effects by inhibiting Mps1 phosphorylation and inducing DNA damage [1].

Mps1-IN-6 (Compound 9) is a highly effective Mps1 inhibitor with an IC50 value of 6.4 nM and exhibits significant anti-proliferation and anti-tumor effects on breast cancer cells.

Mps1-IN-6, a potent Mps1 inhibitor, demonstrates antiproliferative and antitumor activities with an IC50 of 2.596 nM [1].

Mps1-IN-8, a Mps1 inhibitor, can be utilized in the study of various tumors [1].

BAY 1217389 is an effective and selective inhibitor of the monopolar spindle 1 (MPS1) kinase (IC50<10 nM).

NMS-P715 is a selective and ATP-competitive MPS1 inhibitor(IC50 of 182 nM).

CCT251455, the mitotic kinase monopolar spindle 1 (MPS1 TTK) inhibitor, is a potent (IC50=3 nM) and specific chemical tool.

PF-3837 is an inhibitor of the Mps1 kinase, with a Ki value of 0.33 nM and an IC50 value of 5.5 nM. It disrupts cell cycle checkpoints by inhibiting the catalytic activity of Mps1, thereby reducing genomic stability and leading to cancer cell apoptosis (Apoptosis). PF-3837 is utilized in the study of breast cancer.

ONCOII, an inhibitor of Mps1 with an IC50 of 10.8 nM, exhibits varying inhibitory activities depending on naturally occurring mutations within the Mps1 gene. Cells harboring Mps1 mutations demonstrate increased resistance to ONCOII. This compound is applicable in cancer research.

PF-7006, an Mps1 kinase inhibitor, exhibits a Ki value of 0.27 nM and an IC50 value of 2.5 nM. It disrupts cell cycle checkpoints by inhibiting the catalytic activity of Mps1, reduces histone H3 levels, and shortens the duration of mitosis, thereby inducing apoptosis (Apoptosis) in cancer cells. When used in combination with Palbociclib, the tolerance of cancer cells to PF-7006 is enhanced. PF-7006 is applicable for research on breast cancer.