"目录号: HY-15217
CHR-6494是Haspin(单倍体生殖细胞特异性核蛋白激酶)抑制剂,能阻断H3T3ph的磷酸化。
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Description
CHR-6494 is a potent and selective Haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase) inhibitor that blocks H3T3ph phosphorylation. IC50 Value: N/ATarget: Haspin KinaseCHR-6494 is a first-in-class Haspin inhibitor with a wide spectrum of anticancer effects. Recent research showed that CHR-6494 reduces H3T3ph levels in a dose-dependent manner and causes a mitotic catastrophe characterized by metaphase misalignment, spindle abnormalities and centrosome amplification. From the cellular standpoint, the identified small-molecule Haspin inhibitor causes arrest in G2/M and subsequently apoptosis. Importantly, ex vivo assays also demonstrate its anti-angiogenetic features; in vivo, it shows antitumor potential in xenografted nude mice without any observed toxicity.
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