LDN-192960 HYDROCHLORIDE

IC50: 10 nM (Haspin); 48 nM (DYRK2)

LDN-192960 hydrochloride (10 μM) is selective and inhibits ten of the other kinases by ≥90%, with only five being potently inhibited (IC ₅₀ <1 μM), including CLK1 (IC ₅₀ =0.21 μM), DYRK1A (IC ₅₀ = 0.10 μM), DYRK2 (IC ₅₀ =2 nM), DYRK3 (IC ₅₀ =19 nM) and PIM1 (IC ₅₀ =0.72 μM).LDN-0192960 hydrochloride (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 EC ₅₀ of 1.17 μM.LDN-0192960 hydrochloride (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 EC ₅₀ of 0.02 μM.