Hesperadin

Category	Influenza Virus
CAS	422513-13-1
Description	Hesperadin is an inhibitor of human Aurora B, which can prevent the phosphorylation of substrate with IC(50) of 40 nM. Growth of cultured bloodstream forms was also sensitive to Hesperadin (IC(50) of 50 nM). Hesperadin blocked nuclear division and cytokinesis but not other aspects of the cell cycle. Consequently, growth arrested cells accumulated multiple kinetoplasts, flagella and nucleoli, similar to the effects of RNAi-dependent knockdown of TbAUK1 in cultured bloodstream forms cells. Molecular models predicted high-affinity binding of Hesperadin to both conserved and novel sites in TbAUK1. Collectively, these data demonstrate that cell cycle progression is essential for infections with T. brucei and that parasite Aurora kinases can be targeted with small-molecule inhibitors.

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Product Information

Synonyms	Hesperadin
Molecular Weight	516.65
Molecular Formula	C29H32N4O3S
Canonical SMILES	CCS(=O)(=O)NC1=CC2=C(C=C1)NC(=O)C2=C(C3=CC=CC=C3)NC4=CC=C(C=C4)CN5CCCCC5
InChI	InChI=1S/C29H32N4O3S/c1-2-37(35,36)32-24-15-16-26-25(19-24)27(29(34)31-26)28(22-9-5-3-6-10-22)30-23-13-11-21(12-14-23)20-33-17-7-4-8-18-33/h3,5-6,9-16,19,30,32H,2,4,7-8,17-18,20H2,1H3,(H,31,34)/b28-27-
InChIKey	GLDSKRNGVVYJAB-DQSJHHFOSA-N
Purity	≥98% (HPLC)
Density	1.3±0.1 g/cm3
Solubility	In Vitro: DMSO : ≥ 100 mg/mL(193.55 mM) In Vivo: 1.Add each solvent one by one:10% DMSO >> 40%PEG300 >> 5%Tween-80 >> 45% saline Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution 2.Add each solvent one by one:10% DMSO >> 90%corn oil Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution
Appearance	white solid powder
Storage	Powder: -20°C: 3 years 4°C: 2 years In solvent: -80°C: 6 months -20°C: 1 month
Complexity	855
Exact Mass	516.21951207
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
XLogP3-AA	5.2