Hesperadin

Research use only, not for human use.

Hesperadin is a small molecule Aurora B inhibitor (IC50=250 nM) that perturbs mitosis and induces polyploidy.

Hesperadin is a small molecule Aurora B inhibitor (IC50=250 nM) that perturbs mitosis and induces polyploidy, causes mammalian cells to enter anaphase in the presence of monooriented chromosomes; inhibits histone H3 phosphorylation and causes midspindle defects, but does not inhibit APC and separase activation; also markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1, and PHK 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. Cell Viability Assay Cell Line:M110 cells Concentration:0.01, 0.1, 1, 10 μM Incubation Time:24 hours or 48 hours Result:Inhibiting growth of BF cultures with IC50 of 50 nM, while the inhibition of PF growth required approximately 11-fold more Hesperadin, with IC50 of 550 nM.Cell Cycle Analysis Cell Line:M110 cells Concentration:100, 200 nM Incubation Time:24, 48, 72 hours Result:Had a strong effect on cell growth and mitotic progression at 100-200 nM.

Hesperadin (20 mg/kg/d; i.v.) prolongs the survival of xenograft mice via synergistic effect with temozolomide (TMZ). Animal Model:6-week-old female nude mice injected GBM cells Dosage:20 mg/kg/d Administration:I.v. injection Result:Increased the survival of xenograft mice models.

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Cell Cycle/DNA Damage

Aurora Kinase

AuroraB(human)|TbAUK1

Cancer

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422513-13-1

516.6544

C29H32N4O3S

>98% (HPLC)

10 mM in DMSO

CCS(=O)(=O)NC1=CC2=C(C=C1)NC(=C2C(=NC3=CC=C(C=C3)CN4CCCCC4)C5=CC=CC=C5)O

Ethanesulfonamide, N-[2,3-dihydro-2-oxo-3-[(3Z)-phenyl[[4-(1-piperidinylmethyl)phenyl]amino]methylene]-1H-indol-5-yl]-

(-20℃)

With Ice Pack

≥ 2 years