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LDN-192960
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LDN-192960图片
CAS NO:184582-62-5
包装:5mg
规格:98%
市场价:1872元
分子量:328.43

产品介绍
LDN-192960是一种有效的Haspin(单倍体生殖细胞特异性核蛋白激酶)抑制剂,其IC50值为0.010μM。
CAS:184582-62-5
分子式:C18H20N2O2S
分子量:328.43
纯度:98%
存储:Store at -20°C

Background:

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.