MilliporeSigma™ Calbiochem™ Haspin Kinase Inhibitor, CHR-6494

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.).

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