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AZ3146 is a novel Mps1 inhibitor with IC50 of 35 nM. AZ3146 significantly inhibits phosphorylation of Mps1 in cells. AZ3146 displays selectivity over 46 other kinases including Cdk1 and aurora kinase B. AZ3146 also inhibits the recruitment of Mad1, Mad2 and centromere protein E (CENP-E) to kinetochores. AZ3146 has a dramatic effect on kinetochore localization of Mad2, reducing its levels to ~15%, but its effect on Mad1 is less pronounced, with levels remaining at ~60%.
| Molecular Weight | 452.55 |
| Formula | C24H32N6O3 |
| CAS Number | 1124329-14-1 |
| Solubility (25°C) | DMSO 25 mg/mL Ethanol 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Kinesin Products |
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| Ispinesib
Ispinesib (SB 715992) is the first potent, highly specific small-molecule inhibitor of kinesin spindle protein (KSP) with an IC50 of 4.1 nM. |
| SB-743921
SB-743921 is a highly potent and active KSP inhibitor with a Ki of 0.1 nM for KSP (Eg5). |
| GSK923295
GSK923295 is an allosteric inhibitor of CENP-E with Ki value of 3.2 nM. |
| 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. |
| ARRY-520
ARRY-520 is a potent and selective kinesin spindle protein (KSP) inhibitor with an IC50 of 15 nM for A2780, CP70 and 01-28 cell lines in vitro. |
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