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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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| AZD4877
AZD4877 is another isostere to Ispinesiband also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. |
| Filanesib TFA
Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. |
| Filanesib hydrochloride
Filanesib (ARRY-520) hydrochloride is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. |
| Eg5-IN-1
Eg5-IN-1 is a potent kinesin family motor protein (Eg5) inhibitor with an IC50 value of 1.97 µM. |
| PVZB-1194
PVZB-1194 is a biphenyl-type inhibitor of kinesin Eg5 that induces apoptosis by inhibiting Eg5 ATPase activity and shows potent kinesin spindle protein (KSP) inhibition only in the presence of microtubules, with anticancer activity. |
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