Mps1 Inhibitor

TTK inhibitor 3 is a potent and selective TTK (an essential spindle assembly checkpoint enzyme) inhibitor with an IC₅₀ value of 3.0 nM.

Mps-BAY1 is an MPS1 inhibitor with anticancer activity. Mps-BAY1 inhibits cell proliferation and induces apoptosis by activating mitotic catastrophe in cancer cells, generating global aneuploidy and polyploidy. Mps-BAY1 can be used in the study of colorectal cancer and cervical cancer.

Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC₅₀ value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage.

CFI-401870 is an orally active threonine tyrosine kinase (TTK (Mps1)) inhibitor with an IC₅₀ of 3.1 nM. CFI-401870 exhibits IC₅₀s against PLK4, KDR, AURKA and other kinases such as AURKB/INCENP were all greater than 1 μM.CFI-401870 inhibits the growth of various cancer cells, causing chromosome lag, an increase in aneuploidy and cell cycle arrest. CFI-401870 can be used for the study of cancers such as colon cancer.

Mps1-IN-1 dihydrochloride is a potent and ATP-competitive Mps1 kinase inhibitor with an IC₅₀ of 367 nM. Mps1-IN-1 dihydrochloride inhibit Mps1 mitotic kinase activity and abrogates spindle assembly checkpoint (SAC) function. Mps1-IN-1 dihydrochloride decreases the viability of both cancer and ‘normal’ cells.

Mps1-IN-6 is a potent Mps1 inhibitor with an IC₅₀ value of 2.596 nM. Mps1-IN-6 shows antiproliferative activity. Mps1-IN-6 shows antitumor activity.

TTK/PLK1-IN-1 (Formula I) is the inhibitor for threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1) with IC₅₀ of 7 nM and 72 nM. TTK/PLK1-IN-1 regulates spindle assembly checkpoint (SAC), and exhibits antitumor efficacy against TNBC.

TTK-IN-5 is an orally active covalent threonine tyrosine kinase (TTK) inhibitor with selectivity (IC₅₀ = 8.918 nM). TTK-IN-5 exhibits anti-proliferative potencies against MDA-MB-231, A2780, HCT116, HCC1569 and MKN1 cell lines (IC₅₀ values of 0.113 μM, 0.476 μM, 3.136 μM, 3.649 μM, and 1.856 μM, respectively). TTK-IN-5 potently suppresses tumor growth without notable toxicity in A2780 and MDA-MB-231 xenograft mouse models. TTK-IN-5 can be used for the research of cancer such as breast cancer and ovarian cancer.

Mps1-IN-4 is a selective Monopolar spindle 1 (Mps1) inhibitor with antiproliferative activity for cancer research.

TTK inhibitor 4 (compound 16) is a potent inhibitor of threonine tyrosine kinase (TTK), with the IC₅₀ value of 0.016 μM, that has anti-tumor activity.

CFI-401980 is a selective tyrosine threonine kinase MPS1 inhibitor with a K_i of 0.8 nM. CFI-401980 inhibits the proliferation of HCT116 cell lines. CFI-401980 can be studied in anti-cancer research.

Mps1-IN-8 is a Mps1 inhibitor. Mps1-IN-8 can be used in the study of various tumors.

CFI-400936 is a potent TTK inhibitor with an IC₅₀ of 3.6 nM. CFI-400936 has antitumor activity.

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.

PF-3837 is an Mps1 kinase inhibitor with a K_i 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.

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.

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-BAY2a (Standard) is the analytical standard of Mps-BAY2a (HY-110242). This product is intended for research and analytical applications. Mps-BAY2a is a monopolar spindle 1 (MPS1) inhibitor with an IC₅₀ of 1 nM against human MPS1. Mps-BAY2a induces mitotic aberrations and apoptosis in cancer cells.

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 K_d 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 K_d 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.

PF-7006 is an Mps1 kinase inhibitor with a K_i 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.