LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC 50 s of 10 nM and 48 nM, respectively
In Vitro
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
