1124329-14-1

AZ3146 (1124329-14-1) is a potent (IC50?= 35 nM) and selective monopolar spindle 1 (Mps1/TTK) kinase inhibitor.1?Mps1 has an essential role in the spindle assembly checkpoint, an inhibitory network that restrains anaphase until all kinetochores are stably attached to spindle microtubules during mitosis. AZ3146 decreased hepatocellular carcinoma growth in vitro (SMMC-7721 and BEL-7404 cells).2

AZ 3146 is a protein kinase Mps1 inhibitor.

This selective inhibitor (FW = 452.55 g/mL; CAS 1124329-14-1; Solubility: 28 mg/mL DMSO; <1 mg/mL Water), also known as 9- cyclopentyl-2- (2-methoxy-4- (1-methylpiperidin-4-yloxy) phenylamino) -7- methyl-7H-purin-8 (9H) -one, inhibits MPS1 protein kinases (IC50 = 35 nM), which are found widely, but not ubiquitously, in eukaryotes and regulate kinetochore in both the chromosome attachment and the spindle checkpoints. MPS1 kinases also regulate centrosome function.

Mps1^Cat: 35 nM (IC₅₀)

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1) Hewitt?et al. (2010)?Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex; J. Cell Biol.?190?25 2) Liu?et al.?(2015)?TTK activates Akt and promotes proliferation and migration of hepatocellular carcinoma cells; Oncotarget?6?34309