HesperadinHesperadin
MedChemExpress (MCE)
HY-12054
422513-13-1
98.00%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.
Hesperadin (10-100 nM) inhibits the Aurora kinase-1 (TbAUK1)-mediated phosphoryation of trypanosome histone H3 (TbH3) in a dose dependent manner, with an IC50 of 40 nM[1]. Hesperadin (0.01-10 μM
24 or 48 hours) inhibits growth of bloodstream forms (BF) and procyclic forms (PF) cultures[1]. Hesperadin (100-200 nM
24-72 hours) alters cell morphology and inhibits cell cycle progression similar to the RNAi knockdown of TbAUK1[1].
Hesperadin (20 mg/kg/d
i.v.) prolongs the survival of xenograft mice via synergistic effect with temozolomide (TMZ)[2].
Trypanosoma Aurora B 250 nM (IC50)
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[1]. Neal J, et, al. The cell cycle as a therapeutic target against Trypanosoma brucei: Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms. Mol Microbiol. 2009 Apr
72(2): 442-58. [Content Brief]
[2]. Wahafu A, et, al. Targeting Aurora kinase B attenuates chemoresistance in glioblastoma via a synergistic manner with temozolomide. Pathol Res Pract. 2019 Nov
215(11): 152617. [Content Brief]
[3]. Hu Y, et, al. Chemical Genomics Approach Leads to the Identification of Hesperadin, an Aurora B Kinase Inhibitor, as a Broad-Spectrum Influenza Antiviral. Int J Mol Sci. 2017 Sep 8
18(9):1929. [Content Brief]