| S2731 |
AZ 3146
|
AZ3146 is a selective Mps1 inhibitor with IC50 of ~35 nM, contributes to recruitment of CENP-E (kinesin-related motor protein), less potent to FAK, JNK1, JNK2, and Kit.
|
-
Cell Rep Med, 2025, 6(6):102160
-
EMBO J, 2025, 44(13):3794-3823
-
J Cell Biol, 2025, 224(6)e202409219
|
|
| S7488 |
MPI-0479605
|
MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 with IC50 of 1.8 nM, >40-fold selectivity over other kinases.
|
-
Adv Sci (Weinh), 2025, 12(45):e07839
-
Sci Rep, 2024, 14(1):15912
-
Mol Biol Cell, 2024, 35(8):br15
|
|
| S8215 |
BAY 1217389
|
BAY 1217389 is an orally bioavailable, selective inhibitor of the serine/threonine kinase monopolar spindle 1 (Mps1) with IC50 values below 10 nmol/L while showing an excellent selectivity profile.
|
-
Sci Rep, 2024, 14(1):15912
-
Nat Commun, 2023, 10.1038/s41467-023-43274-3
-
Dev Cell, 2023, 58(3):192-210.e11
|
|
| S8214 |
Empesertib (BAY1161909)
|
Empesertib (BAY1161909, Mps1-IN-5), a derivative of triazolopyridine, is an orally bioavailable, selective inhibitor of the serine/threonine monopolar spindle 1 (Mps1) kinase with IC50 of <1 nM. This compound has potential antineoplastic activity.
|
-
Commun Biol, 2025, 8(1):1011
-
Sci Adv, 2023, 9(3):eadd6982
|
|
| S8911 |
BOS172722
|
BOS172722 is a monopolar spindle 1 (MPS1) checkpoint inhibitor with IC50 of 11 nM, Ki of 0.11 nM.
|
-
Cancer Res, 2025, 85(15):2921-2938
-
Cancer Res, 2025, 10.1158/0008-5472.CAN-25-0999
|
|
| E1428 |
Mps1-IN-6 (Compound 9)
|
Mps1-IN-6 (Compound 9) is a potent Mps1 inhibitor with IC50 of 6.4 nM. It also exhibits antiproliferative and anti-tumor activity in breast cancer cells.
|
|
|
| S6768 |
CC-671
|
CC-671 is a selectively dual inhibitor of TTK (human protein kinase monopolar spindle 1 [hMps1]) and CDC like kinase 2 (CLK2) with IC50s of 5 nM and 3 nM for TTK and CLK2, respectively.
|
|
|