"目录号: HY-15217
Cell Cycle/DNA Damage-
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。
Haspin Kinase
相关产品
生物活性
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.
References
[1].Cuny, Gregory D.; Ulyanova, Natalia P.; Patnaik, Debasis et al. Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. Bioorganic & Medicinal Chemistry Letters (2012), 22(5), 2015-2019.
[2].Huertas, D.; Soler, M.; Moreto, J. et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene (2012), 31(11), 1408-1418.
[3].Wang F, Ulyanova NP, Daum JR et al. Haspin inhibitors reveal centromeric functions of Aurora B in chromosome segregation. J Cell Biol. 2012 Oct 15;199(2):251-68.