Mps1 Inhibitor

BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC₅₀ value less than 10 nM.

CFI-402257 is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC₅₀ of 1.7 nM for TTK in vitro. CFI-402257 has anti-cancer activity.

AZ3146 is a reasonably potent Mps1 and TTK inhibitor, with IC₅₀ of 35 nM for Mps1^Cat.

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.

NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC₅₀ of 182 nM.

LRRK2-IN-21 is a selective, blood-brain barrier-permeable LRRK2 kinase inhibitor with an IC₅₀ of 0.35 nM. LRRK2-IN-21 inhibits TTK kinase with an IC₅₀ of 70 nM. LRRK2-IN-21 is applicable to the research of Parkinson's disease.

MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC₅₀ of 1.8 nM.

Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC₅₀ of 50 nM.

dAurAB5 is a dual Aurora-A (DC₅₀ = 8.8 nM) and Aurora-B (DC₅₀ = 6.1 nM) PROTAC degrader. dAurAB5 induces degradation of Aurora-A and Aurora-B, reduces N-Myc levels, and decreases viability in IMR32 neuroblastoma cells. dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. dAurAB5 can be used to study cancers such as neuroblastoma. (Pink: TTK ligand 2: HY-168542, Blue: Thalidomide-O-COOH: HY-103597, Black: 6-Aminocaproic acid: HY-B0236).

BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) checkpoint with an IC₅₀ of 11 nM and 63 nM for MPS1 (1 mM ATP) and P-MPS1, respectively. BOS-172722 also has potential for the study of various forms of breast cancer.

Empesertib (BAY 1161909) is a potent Mps1 inhibitor, with an IC₅₀ of < 1 nM.

Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC₅₀ and a K_d of 367 nM and 27 nM.

NTRC 0066-0 is a selective threonine tyrosine kinase (TTK) inhibitor (IC₅₀=0.9 nM). NTRC 0066-0 can be used for the research of cancer.

TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC₅₀ of 6.4 nM.

Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC₅₀ and a K_d of 145 nM and 12 nM for Mps1 and a K_d of 61 nM for Plk1.

CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 (MPS1) inhibitor with an IC₅₀ of 3 nM.

RMS-07 is a covalent Monopolar Spindle Kinase 1 (MPS1/TTK) inhibitor, with an apparent IC₅₀ of 13.1 nM. RMS-07 targets a poorly conserved cysteine in the kinase's hinge region.

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-IN-7 is a potent MPS1 inhibitor (IC₅₀ of 0.020 μM) over JNK1 and JNK2 (JNK1 IC₅₀= 0.11 μM, JNK2 IC₅₀=0.22 μM). Mps1-IN-7 inhibit SW620, CAL51, Miapaca-2, RMG1 cell growth with GI₅₀ values of 0.065, 0.068, 0.25, and 0.110 μM,respectively.

Mps1-IN-3 hydrochloride is a potent and selective Mps1 inhibitor with an IC₅₀ value of 50 nM. Mps1-IN-3 hydrochloride can inhibit the proliferation of glioblastoma cells, and effectively sensitizes glioblastomas to Vincristine in orthotopic glioblastoma xenograft model.