A multi-kinase inhibitor
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Hesperadin

Item No. 24199

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2,3-dihydro-2-oxo-3-[(3Z)-phenyl[[4-(1-piperidinylmethyl)phenyl]amino]methylene]-1H-indol-5-yl]-ethanesulfonamide
CAS Number
422513-13-1
Molecular Formula
C29H32N4O3S
Formula Weight
516.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMSO: 33 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml
λmax
287, 378 nm
SMILES
O=C(NC1=C/2C=C(NS(CC)(=O)=O)C=C1)C2=C(NC3=CC=C(CN4CCCCC4)C=C3)\C5=CC=CC=C5
InChi Code
InChI=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-
InChi Key
GLDSKRNGVVYJAB-DQSJHHFOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Hesperadin is a multi-kinase inhibitor.1,2,3 It inhibits human Aurora kinase B (IC50 = 250 nM) and its T. brucei homolog Aurora kinase-1 (IC50 = 40 nM) in in vitro kinase assays.1,2 Hesperadin (1 µM) inhibits AMPK, LCK, MKK1, MAPKAP-K1, CHK1, and PHK in a panel of 25 kinases.1 It also inhibits MEKK2 in ATPase and transphosphorylation assays with IC50s of 60 and 34 nM, respectively.3 Hesperadin (50-100 nM) induces polyploidy and defects in cytokinesis and spindle assembly as well as inhibits proliferation of HeLa cells and overrides mitotic arrest induced by paclitaxel (Item No. 10461) or monastrol (Item No. 15044).1 Hesperadin also induces toxicity in HepG2 cells with a toxic concentration (TC50) value of less than 0.2 µM.4 It inhibits replication of clinical isolates of influenza A and B viruses with EC50s ranging from 0.22 to 2.21 µM in a plaque formation assay.5 Hesperadin inhibits the growth of T. brucei, L. major promastigotes and amastigotes, and P. falciparum with EC50 values ranging from 0.01 to 2.37 µM, but has less activity against T. cruzi (EC50 = 39 µM).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hauf, S., Cole, R.W., LaTerra, S., et al. The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint. J. Cell. Biol. 161(2), 281-294 (2003).

    2. Jetton, N., Rothberg, K.G., Hubbard, J.G., et al. The cell cycle as a therapeutic target against Trypanosoma brucei: Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms. Mol. Microbiol. 72(2), 442-458 (2009).

    3. Girdler, F., Gascoigne, K.E., Eyers, P.A., et al. Validating Aurora B as an anti-cancer drug target. J. Cell Sci. 119(Pt 17), 3664-3675 (2006).

    4. Patel, G., Roncal, N.E., Lee, P.J., et al. Repurposing human Aurora kinase inhibitors as leads for anti-protozoan drug discovery. Medchemcomm. 5(5), 655-658 (2014).

    5. Hu, Y., Zhang, J., Musharrafieh, R., et al. Chemical genomics approach leads to the identification of hesperadin, an Aurora B kinase inhibitor, as a broad-spectrum influenza antiviral. Int. J. Mol. Sci. 18(9), pii: E1929 (2017).