Hesperadin - CAS 422513-13-1
Catalog number:
422513-13-1
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
Aurora Kinase
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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Appearance:
white solid powder
Synonyms:
Hesperadin
MSDS:
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1.Synthesis and investigation of new Hesperadin analogues antitumor effects on HeLa cells.
Shamsipour F1, Hosseinzadeh S2, Arab SS3, Vafaei S1, Farid S1, Jeddi-Tehrani M1, Balalaie S2. J Chem Biol. 2014 May 18;7(3):85-91. doi: 10.1007/s12154-014-0111-3. eCollection 2014.
Hesperadin is one of the indolinones that was designed against the ATP-binding site of Aurora kinase. This molecule inhibits Aurora B kinase by phosphorylation of histone H3. In this study, new derivatives of Hesperadin containing an amide group in their structures were synthesized through sequential Ugi/palladium-catalyzed approach and in vitro antitumor activity of new compounds were evaluated by cell proliferation assay. The results show that compounds 6f, 6i, 6l, and 6o were dose-dependently inhibited in different concentrations, and IC50 values were between 35 and 43 nM. It seems that lipophilic substitution on the indolinone core with the ability to form additional hydrogen bond might lead to increased stability of structure and activity of new Hesperadin analogues.
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CAS 422513-13-1 Hesperadin

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