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Hesperadin

Catalog No.: 17011902
Cas No.: 422513-13-1
Purity : 98% 
17011902 - Hesperadin | CAS 422513-13-1

Catalog number : 17011902

CAS number : 422513-13-1

Molecular Formula : C29H32N4O3S 

Molecular Weight : 516.65 

Iupac Chemical Name : (Z)-N-(2-oxo-3-(phenyl((4-(piperidin-1-ylmethyl)phenyl)amino)methylene)indolin-5-yl)ethanesulfonamide 

Smile : O=C\1NC2=CC=C(C=C2/C1=C(/NC1=CC=C(C=C1)CN1CCCCC1)\C1=CC=CC=C1)NS(=O)(=O)CC

InChiKey : GLDSKRNGVVYJAB-DQSJHHFOSA-N

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SynonymsN/A 
Molecular FormulaC29H32N4O3S 
Molecular Weight516.65 
Appearancecrystalline solid 
Purity98% 
SolubilitySoluble in DMSO 
Storage3 years -20ºCpowder 
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. 
SmileO=C\1NC2=CC=C(C=C2/C1=C(/NC1=CC=C(C=C1)CN1CCCCC1)\C1=CC=CC=C1)NS(=O)(=O)CC
InChiKeyGLDSKRNGVVYJAB-DQSJHHFOSA-N
InChiInChI=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-
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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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