mps1 in 1

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

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-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-10 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-3 is an effective and selective inhibitor of MPS1 kinase (IC50: 50 nM).

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

CFI-402257 (Luvixasertib) is a highly selective oral TTK (Mps1, Monopolar Spindle 1) kinase inhibitor that potently inhibits TTK kinase activity (Mps1 Ki = 0.09 nM；EC50 = 6.5 nM). It is intended for use in research on hepatocellular carcinoma and breast cancer.

DW532 is one of simplified analogues of hematoxylin that has shown broad-spectrum inhibition on tyrosine kinases and in vitro anti-cancer activities. DW532 inhibited EGFR and VEGFR2 in vitro kinase activity (the IC50 values were 4.9 and 5.5 μmol/L, respectively), and suppressed their downstream signaling. DW532 dose-dependently inhibited tubulin polymerization via direct binding to tubulin, thus disrupting the mitotic spindle assembly and leading to abnormal cell division. In a panel of human cancer cells, DW532 (1 and 10 μmol/L) induced G2/M phase arrest and cell apoptosis, which subsequently resulted in cytotoxicity. Knockdown of BubR1 or Mps1, the two core proteins of the spindle assembly checkpoint dramatically decreased DW532-induced cell cycle arrest in MDA-MB-468 cells. Moreover, treatment with DW532 potently and dose-dependently suppressed angiogenesis in vitro and in vivo. ( Acta Pharmacol Sin. 2014 Jul;35(7):916-28.)

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].

RMS-07, a covalent inhibitor of Monopolar Spindle Kinase 1 (MPS1/TTK), exhibits a potent inhibitory concentration (IC50) of 13.1 nM. Specifically, it targets a poorly conserved cysteine located in the hinge region of the kinase.

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

CFI-402257 hydrochloride, a highly selective and orally bioavailable inhibitor targeting TTK/Mps1, demonstrates an in vitro IC50 value of 1.7 nM against TTK. This compound exhibits anti-cancer activity [1].

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