LDN-192960 is an inhibitor of both Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2), exhibiting IC50 values of 10 nM and 48 nM, respectively [1].
体外研究
At a concentration of 10 μM, LDN-192960 exhibits selectivity and inhibits over 90% of ten other kinases, with only five showing potent inhibition (IC50<1 μM), including CLK1 (IC50=0.21 μM).
LDN-0192960 (0-5 μM; 2 hours) exhibits the characteristic inhibition profile of Haspin by decreasing p-Thr3H3 levels in HeLa cells overexpressing Haspin, with an EC50 of 1.17 μM [2].
LDN-0192960 (0-1 μM; 1 hour incubation in the presence of nocodazole and MG132) demonstrates the typical Haspin inhibition pattern by reducing p-Thr3H3 levels in mitotically synchronized HeLa cells, with an EC50 of 0.02 μM [2].
LDN-192960 细胞实验
Cell Line
Concentration
Treated Time
Description
References
5TGM1
3 μM
48 hours
LDN192960 in combination with TIR-199 showed remarkable synergistic cytotoxicity in 5TGM1 cells.
Biosci Rep. 2022 Feb 25;42(2):BSR20212721
MPC11
5 μM
48 hours
LDN192960 in combination with TIR-199 showed remarkable synergistic cytotoxicity in MPC11 cells.
Biosci Rep. 2022 Feb 25;42(2):BSR20212721
MM.1S
3 μM
48 hours
LDN192960 in combination with TIR-199 showed a modest additive impairment of proteasome activity in MM.1S cells and induced remarkable synergistic cytotoxicity in MPC11 and 5TGM1 cells.
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