Hesperadin-hydrochloride

Category	Influenza Virus
Description	Hesperadin hydrochloride is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin hydrochloride inhibits Aurora B with an IC50 of 250 nM.

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Synonyms	Hesperadin hydrochloride\|Hesperadin (hydrochloride)\|N-[2-hydroxy-3-[C-phenyl-N-[4-(piperidin-1-ylmethyl)phenyl]carbonimidoyl]-1H-indol-5-yl]ethanesulfonamide;hydrochloride\|Hesperadin HCl\|UNII-5JTM1CDL6K\|5JTM1CDL6K\|HY-12054A\|AKOS024457913\|AS-16788\|CS-0120606\|Q27262467\|N-[2,3-Dihydro-2-oxo-3-[(3Z)-phenyl[[4-(1-piperidinylmethyl)phenyl]amino]methylene]-1H-indol-5-yl]-ethanesulfonamide hydrochloride
Molecular Weight	553.12
Molecular Formula	C29H33ClN4O3S
Canonical SMILES	CCS(=O)(=O)NC1=CC2=C(C=C1)NC(=C2C(=NC3=CC=C(C=C3)CN4CCCCC4)C5=CC=CC=C5)O.Cl
Purity	≥98% (HPLC)
Density	1.3±0.1 g/cm3
Solubility	Soluble in DMSO
Appearance	Solid powder
Storage	Store at -20°C
Complexity	855
Exact Mass	552.1961898
Index Of Refraction	1.675
In Vitro	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. Hesperadin (0.01-10 μM; 24 or 48 hours) inhibits growth of bloodstream forms (BF) and procyclic forms (PF) cultures. Hesperadin (100-200 nM; 24-72 hours) alters cell morphology and inhibits cell cycle progression similar to the RNAi knockdown of TbAUK1.
In Vivo	Hesperadin (20 mg/kg/d; i.v.) prolongs the survival of xenograft mice via synergistic effect with temozolomide (TMZ).
PSA	102.41000
Target	Aurora kinase; Autophagy; Influenza Virus; Parasite