Hesperadin , ≥98% , 422513-13-1

Synonym(s):
Hesperadin - CAS 422513-13-1 - Calbiochem;Mammalian Ste20-like Kinase 4 Inhibitor, MST4 Inhibitor, Aurora Kinase Inhibitor X, AMPK Inhibitor II

CAS NO.：422513-13-1

Empirical Formula: C29H32N4O3S

Molecular Weight: 516.65

MDL number: MFCD18074526

EINECS: 200-258-5

PRODUCT Properties

• Melting point: 228 °C
• Density: 1.326
• storage temp.: Refrigerator
• solubility: DMSO, Methanol
• form: Solid
• pka: 9.14±0.20(Predicted)
• color: Yellow
• CAS DataBase Reference: 422513-13-1

Description and Uses

Hesperadin is a multi-kinase inhibitor. 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. Hesperadin (1 μM) inhibits AMPK, LCK, MKK1, MAPKAP-K1, CHK1, and PHK in a panel of 25 kinases. It also inhibits MEKK2 in ATPase and transphosphorylation assays with IC₅₀s of 60 and 34 nM, respectively. 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 or monastrol . Hesperadin also induces toxicity in HepG2 cells with a toxic concentration (TC₅₀) value of less than 0.2 μM. 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. 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).

Hesperadin phosphorylates human mitotic protein complexes that control physiological changes within the cell to allow for proper and successful chromosome segregation. It also targets aurora kinases in cancer treatment, affecting the chromosomes’ regulation during mitosis.