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Hesperadin

Catalog No. T6532   CAS 422513-13-1

Hesperadin(IC50=250 nM) effectively inhibits Aurora B. It potently reduces the activity of AMPK, MAPKAP-K1, MKK1, Lck, CHK1 and PHK, but it could not inhibit MKK1 activity in vivo.

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Hesperadin Chemical Structure
Hesperadin, CAS 422513-13-1
Pack Size Availability Price/USD Quantity
2 mg In stock $ 33.00
5 mg In stock $ 52.00
10 mg In stock $ 77.00
25 mg In stock $ 128.00
50 mg In stock $ 207.00
1 mL * 10 mM (in DMSO) In stock $ 59.00
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Purity: 99.44%
Purity: 98.04%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Hesperadin(IC50=250 nM) effectively inhibits Aurora B. It potently reduces the activity of AMPK, MAPKAP-K1, MKK1, Lck, CHK1 and PHK, but it could not inhibit MKK1 activity in vivo.
Targets&IC50 Aurora B:250 nM
In vitro In HeLa cells, Hesperadin causing defects in mitosis and cytoplasmic division, leading to cell proliferation and polyploidization stopped, because of Aurora B function inhibition during chromosome connection. Addition of 20-100 nM Hesperadin leading to loss of phosphorylation of the mitogenic histone H3 at the Ser10 site. When Hesperadin concentration was 1 μM, other kinases (AMPK, Lck, MKK1, MAPKAP-K1, CHK1, and PHK) activity were significantly reduced.In an in vitro kinase assay, Hesperadin (IC50 = 40 nM) blocked recombinant trypton histone H3 phosphorylation by T. brucei Aurora kinase-1 (TbAUK1) from the pathogenic Trypanosoma brucei. Hesperadin (IC50 = 48 nM) significantly inhibited the growth of cultured infectious blood form (BF) cells, while Hesperadin (IC50 = 550 nM) and weakly inhibited the growth of insect circulation stage (PF) cells.
Kinase Assay For the Aurora B kinase assay, HeLa cells are lysed in a buffer containing 50 mM NaCl, then centrifuging at 13,000 rpm for 20 minutes at 4 °C. Discard supernatant, add 15 mL lysis buffer containing 250 mM NaCl in order to obtain active Aurora B kinase. Centrifuging at low-speed supernatant of the latter extract is used for immunoprecipitation. Monoclonal mouse anti–AIM-1, or mouse anti-HA, is coupled to GammaBind Plus Sepharose, and beads are rotated over-end in the extract for 90 minutes at 4 °C. Beads are washed, aliquoted, and washed in kinase buffer (20 mM Tris, pH 7.5, 150 mM NaCl, 10 mM MgCl2, 1 mM DTT, 10 mM NaF). The kinase assay is performed with 10 μL beads in 20 μL kinase buffer containing 5 μg histone H3, 10 μM ATP, 2.5 μCi [γ-32P]ATP, and different concentrations of Hesperadin for 20 minutes at 37 °C.
Cell Research HeLa cells and PtK1 cells are added Hesperadin 500 nM for 24 and 48 hours.
Molecular Weight 516.65
Formula C29H32N4O3S
CAS No. 422513-13-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55.3 mg/mL (100 mM)

Ethanol: 27.7 mg/mL (50 mM)

TargetMolReferences and Literature

1. Hauf S, et al. J Cell Biol, 2003, 161(2), 281-294. 2. Jetton N, et al. Mol Microbiol, 2009, 72(2), 442-458. 3. Wang J, Yan X, Chen H, et al. Enhanced UV-B radiation affects AUR1 regulation of mitotic spindle morphology leading to aberrant mitosis[J]. Plant Physiology and Biochemistry. 159: 160-170.

TargetMolCitations

1. Wang J, Yan X, Chen H, et al. Enhanced UV-B radiation affects AUR1 regulation of mitotic spindle morphology leading to aberrant mitosis. Plant Physiology and Biochemistry. 159: 160-170.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Kinase Inhibitor Library Anti-Parasitic Compound Library Epigenetics Compound Library Cell Cycle Compound Library Autophagy Compound Library Anti-Viral Compound Library Bioactive Compounds Library Max Anti-Aging Compound Library Anti-Infection Compound Library

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Keywords

Hesperadin 422513-13-1 Autophagy Cell Cycle/Checkpoint Chromatin/Epigenetic Microbiology/Virology Influenza Virus Parasite Aurora Kinase Aurora procyclic forms bloodstream inhibit Inhibitor inhibitor

 

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