Hesperadin

属性

熔点	>226 °C
溶解性	DMSO 103 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
存贮条件	储存温度-20°C
密度	1.3000

描述

产品介绍	Hesperadin是ATP竞争性Aurora B抑制剂，IC50为250 nM。
生化机理	esperadin prevents the phosphorylation of recombinant trypanosome histone H3 by the T. brucei Aurora kinase-1 (TbAUK1) from pathogenic Trypanosoma brucei with IC50 of 40 nM in vitro kinase assays. Hesperadin significantly inhibits cell growth of cultured infectious bloodstream forms (BF) with IC50 of 48 nM, and only weakly inhibits cell growth of insect stage procyclic forms (PF) with IC50 of 550 nM. Hesperadin inhibits the ability of immunoprecipitated Aurora B to phosphorylate histone H3 with IC50 of 250 nM and markedly reduces the activity of other kinases (AMPK, Lck, MKK1, MAPKAP-K1, CHK1, and PHK) at a concentration of 1 μM.
别名	N-(2,3-二氢-2-氧代-3-((3Z)-苯基((4-(1-哌啶基甲基)苯基)氨基)亚甲基)-1H-吲哚-5-基)乙磺酰胺;;hesperadine；N-[2,3-Dihydro-2-oxo-3-[(3Z)-phenyl[[4-(1-piperidinylmethyl)phenyl]amino]methylene]-1H-indol-5-yl]-ethanesulfonamide; N-[(3Z)-2,3-Dihydro-2-oxo-3-[phenyl[[4-(1-piperidinylmethyl)phenyl]amino]methylene]-1H-indol-5-yl]ethanesulfonamide