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Product Name | Haspin Kinase Inhibitor, CHR-6494 |
Description | Purity ~98% (HPLC). 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-3beta, 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 1uM (chicken embryo aortic arch ring assay) and suppresses tumor growth in HCT-116 xenografted mouse model (50mg/kg, i.p.). Formula: C16H16N6 Solubility: DMSO Molar Mass: 292.3 |
Size | 10mg |
Concentration | n/a |
Applications | n/a |
Other Names | Haspin Kinase Inhibitor, CHR-6494 (3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine, Haploid Germ Cell-Specific Nuclear Protein Kinase Inhibitor, CHR-6494, Indazolyl-propylimidazopyridazin-amine) |
Gene, Accession, CAS # | n/a |
Catalog # | 217412 |
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Order / More Info | Haspin Kinase Inhibitor, CHR-6494 from UNITED STATES BIOLOGICAL |
Product Specific References | n/a |
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