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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.
Catalogue Number
531976
Brand Family
Calbiochem®
Synonyms
AZ 3146, AZ-3146, Monopolar Spindle 1 Kinase Inhibitor, AZ3146
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
05-December-2014 JSW
Synonyms
AZ 3146, AZ-3146, Monopolar Spindle 1 Kinase Inhibitor, AZ3146
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.
Form
Purple powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
1124329-14-1
Chemical formula
C₂₄H₃₂N₆O₃
Purity
≥97% by HPLC
Solubility
DMSO (5 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
