Size | Price | Stock |
---|---|---|
5mg | $55 | In-stock |
10mg | $77 | In-stock |
50mg | $286 | In-stock |
100mg | $495 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-10128 |
M.Wt: | 513.59 |
Formula: | C29H31N5O4 |
Purity: | >98 % |
Solubility: | DMSO : 25 mg/mL (48.68 mM; Need ultrasonic) |
ZM-447439 is an aurora kinase inhibitor with IC50s of 110 and 130 nM for aurora A and B, respectively. IC50 & Target: IC50: 110 nM (Aurora A), 130 nM (Aurora B)[1] In Vitro: Cells treated with ZM-447439 progress through interphase, enter mitosis normally, and assemble bipolar spindles. However, chromosome alignment, segregation, and cytokinesis all fail. ZM-447439 inhibits cell division and inhibit mitotic phosphorylation of histone H3. ZM-447439 prevents chromosome alignment and segregation. ZM-447439 compromises spindle checkpoint function. ZM-447439 inhibits kinetochore localization of BubR1, Mad2, and Cenp-E[1]. Inhibition of Aurora kinase by ZM-447439 reduces histone H3 phosphorylation at Ser10 in Hep2 carcinoma cells. Multipolar spindles are induced in these ZM-treated G2/M-arrested cells with accumulation of 4N/8N DNA, similar to cells with genetically suppressed Aurora-B. ZM-447439 treatment induces cell apoptosis. ZM-447439 inhibition of Aurora kinase is potently in association with decrease of Akt phosphorylation at Ser473 and its substrates GSK3α/β phosphorylation at Ser21 and Ser9[2].
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