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MilliporeSigma™ Calbiochem™ Haspin Kinase Inhibitor, CHR-6494

Catalog No. 37204010MG Shop All MilliporeSigma Products
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Description

A cell-permeable indazolylimidazopyridazinamine compound that acts as a potent and reversible inhibitor of histone kinase haspin activity (IC50 = 2nM) with moderate selectivity over TrkA, GSK-3β, PIM1, Cdk1/B and Cdk2/A (% inhibition at 100nM = 58, 48, 36, 34 and 33, respectively) among a panel of 27-kina

A cell-permeable indazolylimidazopyridazinamine compound that acts as a potent and reversible inhibitor of histone kinase haspin activity (IC50 = 2nM) with moderate selectivity over TrkA, GSK-3β, PIM1, Cdk1/B and Cdk2/A (% inhibition at 100nM = 58, 48, 36, 34 and 33, respectively) among a panel of 27-kinases. Shown to block pH3-Thr3, with no effect on pH3-Ser10 and pH3-Ser28, cause mitotic catastrophe, upregulate BUB1 and cyclin B1 levels, and potently induce apoptosis (IC50 = 473, 500 and 752nM in HeLa, HCT-116 and MDA-MB-231 cells, respectively). Further, efficiently blocks bFGF-induced sprouting vessel by 70% at 1μM (chicken embryo aortic arch ring assay) and suppresses tumor growth in HCT-116 xenografted mouse model (50mg/kg, i.p.).
TRUSTED_SUSTAINABILITY

Specifications

Color Off-white
Description 98% by HPLC
CAS 1333377-65-3
Molecular Formula C16H16N6
Formula Weight 292.3g/mol
Solubility DMSO
Content And Storage Protect from light
Form Solid
Quantity 10 mg
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