| Cat. No. |
Product Name |
CAS No. |
Information |
| H2141 |
NTRC 00660
|
1817791-73-3 |
A highly potent, selective inhibitor of checkpoint kinase TTK/Mps1 with IC50 of 0.6 nM; displays >200-fold selectivity over 276 kinases, including Aurora C, PLK1, PLK4; shows very potent anti-proliferative activity on a broad panel of human cancer cell lines (IC50=18- 897 nM); increases the survival in a murine breast cancer model that mimics human TNBC and delays tumor relapse, combined with docetaxel. |
| H2140 |
NMS-P715
|
1202055-32-0 |
NMS-P715 is a potent, selective, orally bioavailable Mps1 inhibitor with IC50 of 8 nM, Ki of 0.99 nM; displays excellent selectivity in vitro against a panel of 60 kinases at 5 uM; selectively reduces cancer cell proliferation, leaving normal cells almost unaffected, promotes massive spindle assembly checkpoint (SAC) in U2OS cells with EC50 of 68 nM; causes a reduction in G1 phase and a flattening in G2/M phase of the cell cycle accompanied by histone H3 dephosphorylation, PARP cleavage, and histone H2AX phosphorylation; inhibits tumor growth in preclinical cancer models. |
| H2139 |
Mps1-IN-3
|
1609584-72-6 |
Mps1-IN-3 is a selective and highly potent Mps1 kinase inhibitor with IC50 of 50 nM; causes mitotic aberrancies in glioblastoma cells and, in combination with vincristine, induces mitotic checkpoint override, increases aneuploidy and augmentes cell death; sensitizes glioblastoma cells to vincristine in orthotopic mouse models, resulting in prolonged survival without toxicity. |
| H2137 |
Mps1 inhibitor 2
|
1228817-38-6 |
Mps1 inhibitor 2 is a potent, selective Mps1 kinase inhibitor with IC50 of 145 nM, demonstrates >1,000-fold selectivity over a panel of 352 kinases with the major exceptions of Gak and Plk1; leads to defects in Mad1 and Mad2 establishment at unattached kinetochores, decreases Aurora B kinase activity, premature mitotic exit and gross aneuploidy, without any evidence of centrosome duplication defects; decreases cancer cell viability. |
| H2136 |
Mps1 inhibitor 1
|
1125593-20-5 |
Mps1 inhibitor 1 is a potent, selective Mps1 kinase inhibitor with IC50 of 367 nM; demonstrates >1,000-fold selectivity over a panel of 352 kinases with the major exceptions of Alk and Ltk; leads to defects in Mad1 and Mad2 establishment at unattached kinetochores, decreases Aurora B kinase activity, premature mitotic exit and gross aneuploidy, without any evidence of centrosome duplication defects; decreases cancer cell viability. |
| H2135 |
MPI-0479605
|
1246529-32-7 |
MPI-0479605 is a potent, selective, ATP competitive inhibitor of Mps1 with IC50 of 1.8 nM; triggers the time-dependent degradation of both cyclin B and securin, decreases BubR1 phosphorylation in nocodazole-arrested cells, blocks apparent autophosphorylation of Mps1 at threonine 676 in HEK293T cells; impairs spindle assembly checkpoint (SAC), resulting in chromosome segregation defects and aneuploidy, induces p53-p21 pathway in an ATM- and ATR-dependent manner; exhibits cytotoxicity across a broad range of tumor cell lines and antitumor activity in human tumor xenografts. |
| H2134 |
Empesertib
|
1443763-60-7 |
Empesertib (BAY-1161909, BAY1161909) is a potent, selective Monopolar spindle 1 (Mps1/TTK) inhibitor with IC50 of 0.34 nM; inhibits only JNK2 and JNK3 more than 50% at 1 uM in Millipore panel (230 kinases); abrogates nocodazole-induced metaphase arrest in HeLa cells with IC50 of 56 nM, inhibits the proliferation of a panel tumor cell lines covering various cancer with mean IC50 of 160 nM; enhances the efficacy of antimitotic cancer drugs and shows potentially overcome resistance in vivo. |
| H2133 |
CFI-402257
|
1610759-22-2 |
A potent and selective Mps1/TTK kinase inhibitor with Ki of 0.1 nM and cellular Mps1 EC50 of 6.5 nM; exhibit effects consistent with Mps1 kinase inhibition, specifically SAC inactivation, leading to chromosome missegregation, aneuploidy, and ultimately cell death; well-tolerated in mouse models of human cancer and orally active. |
| H2132 |
CFI-401980
|
1610676-27-1 |
CFI-401980 is a potent, selective, novel class TTK (Tyrosine Threonine Kinase) inhibitor with Ki of 0.8 nM, HCT116 GI50 of 13 nM; shows exceptional kinase selectivity; demonstrate a strong anti-proliferative activity in a panel of human cancer cell lines (HCT116 GI50
|
| H2131 |
CFI-401870
|
1599460-95-3 |
A potent, selective, orally active Mps1 (TTK) inhibitor with IC50 of 3.1 nM; displays low off-target activity (>500-fold) and microsomal stability; inhibits HCT116 cell growth with GI50 of
|
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