LDN-192960

LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC₅₀s of 10 nM and 48 nM, respectively^[1]. IC50 & Target: IC50: 10 nM (Haspin); 48 nM (DYRK2)^[1] In Vitro: LDN-192960 (10 μM) is selective and inhibits ten of the other kinases by ≥90%, with only five being potently inhibited (IC₅₀<1 μM), including CLK1 (IC₅₀=0.21 μM), DYRK1A (IC₅₀= 0.10 μM), DYRK2 (IC₅₀=2 nM), DYRK3 (IC₅₀=19 nM) and PIM1 (IC₅₀=0.72 μM)^[1].
LDN-0192960 (0-5 μM; 2 hours) demonstrates that the classical Haspin inhibition phenotype by reducing levels of p-Thr3H3 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 classical Haspin inhibition phenotype by reducing levels of p-Thr3H3 in HeLa cells synchronized in mitosis with an EC₅₀ of 0.02 μM^[2].