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Ispinesib

CAS No. : 336113-53-2

MCE 国际站：Ispinesib

产品活性：Ispinesib 是一种特异性的纺锤体驱动蛋白 KSP 抑制剂，K_{i app} 值为 1.7 nM。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton  |  Apoptosis

作用靶点：Kinesin  |  Apoptosis

In Vitro: Ispinesib is a potent, highly specific inhibitor of KSP, with a K_{i app} of 1.7 nM. Ispinesib (150 nM) inhibits BT-474 and MDA-MB-468 cell lines, with GI₅₀s of 45 and 19 nM, respectively. Ispinesib (SB715992, 15 and 30 nM) suppresses the proliferation of PC-3 prostate cancer cell by 48.65% and 52.16%, and induces apoptosis of prostate cancer cell by 1094.88% and 1516.70%, respectively. Ispinesib up regulates genes responsible for apoptosis and cell cycle arrest, and down regulates genes responsible for cell proliferation and survival. The anti-proliferation and pro-apoptotic activities of Ispinesib can be enhanced by genistein.

In Vivo: Ispinesib (SCID, 8 mg/kg; nude, 10 mg/kg, q4d × 3) reduces tumor volume in mice bearing tumor xenografts of ER-positive (MCF7), HER2-positive (KPL4, HCC1954, and BT-474), and triple-negative (MDA-MB-468) breast cancer cells via i.p. one dose every 4 days repeated three times.

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