LDN-192960 |
Catalog No.GC33086 |
LDN-192960 est un inhibiteur de Haspin et de la kinase régulée par la tyrosine À double spécificité (DYRK2) avec des IC50 de 10 nM et 48 nM, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 184582-62-5
Sample solution is provided at 25 µL, 10mM.
LDN-192960 is a potent Haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase) inhibitor with an IC50 of 0.010 µM.
A comparison of the profiles of LDN-192960 (compound 3) and 42 suggests that only six kinases, including haspin, are inhibited by both compounds ≥90% at 10 µM[1]. LDN-192960 alone does not cause detectable mitotic exit in the mitotic (phospho)-protein monoclonal-2 (MPM-2) assay in HeLa cells. In the presence of 1 µM ZM447439, even concentrations as low as 0.1 µM LDN-192960 cause substantial loss of MPM-2 epitopes, and similar results are obtained in the presence of Hesperadin. However, 10 µM LDN-192960 does not cause mitotic exit in combination with Aurora B inhibition, which is consistent with off-target effects at this higher dose[2].
[1]. Cuny GD, et al. Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. Bioorg Med Chem Lett. 2012 Mar 1;22(5):2015-9. [2]. Fangwei Wang, et al. Haspin inhibitors reveal centromeric functions of Aurora B in chromosome segregation. J Cell Biol. 2012 Oct 15; 199(2): 251-268.
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