5.31976

MPS1 Inhibitor III, AZ3146

• Synonym(e): MPS1 Inhibitor III, AZ3146, AZ 3146, AZ-3146, Monopolar Spindle 1 Kinase Inhibitor, AZ3146
• Empirische Formel (Hill-System): C₂₄H₃₂N₆O₃
• CAS-Nummer: 1124329-14-1
• Molekulargewicht: 452.55
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥97% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Wirksamkeit: ~35 nM IC₅₀
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: purple
• Löslichkeit: DMSO: 5 mg/mL
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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. Wirkung

Cell permeable: yes

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable