LDN-192960 是 Haspin 和 DYRK2 的双重抑制剂，IC₅₀ 值分别为 10 nM 和 48 nM。

LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC 50 s of 10 nM and 48 nM, respectively.

Solid

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

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).
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.
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.
has not independently confirmed the accuracy of these methods.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Cuny GD, et al. Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3491-4.
[2]. Katrin Kestav, et al. Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin. Curr Med Chem. 2017;24(21):2276-2293.