5.31976

MPS1 Inhibitor III, AZ3146

• Synonym(s): MPS1 Inhibitor III, AZ3146, AZ 3146, AZ-3146, Monopolar Spindle 1 Kinase Inhibitor, AZ3146
• Empirical Formula (Hill Notation): C₂₄H₃₂N₆O₃
• CAS Number: 1124329-14-1
• Molecular Weight: 452.55
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥97% (HPLC)
• Quality Level: 100
• form: powder
• potency: ~35 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: purple
• solubility: DMSO: 5 mg/mL
• storage temp.: 2-8°C

Description

General description

A cell permeable purinone derivative that acts as a highly potent and selective inhibitor of monopolar spindle 1 kinase (MPS1; IC₅₀ = ~35 nM). Inhibits the phosphorylation of full-length immunoprecipitated human MPS1 and exhibits minimal activity against a panel of 49 other protein kinases. Has much reduced activity against FAK, JNK1, JNK2, and KIT and does not affect the activity of mitotic-specific phosphoforms of Aurora B and BubR1. Induces a significant reduction in time to complete mitosis (from 90 min to 32 min) and causes abnormal mitosis where over 50% of cells enter anaphase without aligning their chromosomes.

A cell permeable purinone derivative that acts as a highly potent and selective inhibitor of monopolar spindle 1 kinase (MPS1; IC₅₀ = ~35 nM). Inhibits the phosphorylation of full-length immunoprecipitated human MPS1 and exhibits minimal activity against a panel of 49 other protein kinases. Has much reduced activity against FAK, JNK1, JNK2, and KIT and does not affect the activity of mitotic-specific phosphoforms of Aurora B and BubR1. Induces a significant reduction in time to complete mitosis (from 90 min to 32 min) and causes abnormal mitosis where over 50% of cells enter anaphase without aligning their chromosomes.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Hewitt, L., et al. 2010. Jour. Cell Biol.190, 25.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable