Home Cell Cycle MPS1 inhibitor AZ 3146

AZ 3146

Catalog No.S2731

For research use only.

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.

AZ 3146 Chemical Structure

CAS No. 1124329-14-1

Selleck's AZ 3146 has been cited by 20 publications

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Biological Activity

Description 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.
Targets
Mps1 [1]
(Cell-free assay)
~35 nM
In vitro

AZ3146 also inhibits FAK, JNK1, JNK2 and Kit. AZ3146 significantly inhibits phosphorylation of Mps1 in cells. Mitotic-specific phospho forms of aurora B and BubR1 are not affected by AZ3146. AZ3146 does not inhibit Cdk1 or aurora B in mitotic cells. HeLa cells treated with nocodazole and 2 μM AZ3146 only delay mitosis briefly and then rereplicate their genomes, indicating that AZ3146 overrides the SAC. AZ3146 also inhibits an already established SAC signal, as after release from a nocodazole block, AZ3146 dramatically accelerates mitotic exit.During an otherwise unperturbed mitosis, AZ3146 reduces the time to complete mitosis from 90 minutes in controls to 32 minutes. Strikingly, ~90% of AZ3146-treated HeLa cells undergo abnormal mitoses, although ~50% enter anaphase without aligning all of their chromosomes, and ~30% exit mitosis without undergoing obvious chromosome segregation. 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%. When Mps1 is inhibited by AZ3146 before mitotic entry, subsequent recruitment of Mad1 and Mad2 to kinetochores is abolished. However, if Mps1 is inhibited by AZ3146 after mitotic entry, the Mad1–C-Mad2 core complex remains kinetochore bound, but O-Mad2 is not recruited to the core. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
sf9 insect cells NUfMVpZGTnWwY4Tpc44h[XO|YYm= MknlTY5pcWKrdHnvckBw\iCQLYTldo1qdmGuIE\YTIl{NXSjZ3fl[E9IW1RvdHHn[4VlKG[3bHygcIVv\3SqIHj1cYFvKE2SU{Gg[ZhxemW|c3XkJIlvKHKnY3;tZolv[W62IHLhZ5Vtd3[rcoXzJIlv\mWldHXkJJNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiNV\BUU1FUFSJRlzUSXlXSVSUQ1;OTFIh[XNic4Xid5Rz[XSnIHHmeIVzKDZyIITvJFkxKG2rboOgZpkh\my3b4Lld4NmdmOnIHHzd4F6NCCLQ{WwQVchdk1? Mn3NNlQzPTZ{MUe=
human HCT116 cells M1KzW2Z2dmO2aX;uJIF{e2G7 MYPJcohq[mm2aX;uJI9nKE27Yz30ZYdo\WRid3ns[EB1gXCnIF3QV|Eh[XW2b4Doc5NxcG:{eXzheIlwdiCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZYZ1\XJiMjDodpMhcW5icILld4Vv[2Vib3[gdJJwfGWxc3;t[UBqdmirYnn0c5IhVUdzM{KsJGlEPTB;MD63NkDPxE1? MnviNlQzPTZ{MUe=
human HCT116 cells MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmfBO|IhcA>? M1;Rcmdzd3e2aDDpcohq[mm2aX;uJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVEvOiEQvF2= MmnrNlQzPTZ{MUe=
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot Mps1 20624899

Protocol (from reference)

Solubility (25°C)

In vitro

 Ethanol 91 mg/mL
(201.08 mM)
DMSO 28 mg/mL
(61.87 mM)
Water Insoluble

Chemical Information

Molecular Weight 452.55
Formula

C24H32N6O3
CAS No. 1124329-14-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCC(CC1)OC2=CC(=C(C=C2)NC3=NC=C4C(=N3)N(C(=O)N4C)C5CCCC5)OC

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