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: 10 nM (Haspin); 48 nM (DYRK2)^[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

328.43

C₁₈H₂₀N₂O₂S

184582-62-5

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• [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.  [Content Brief]

  [2]. Katrin Kestav, et al. Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin. Curr Med Chem. 2017;24(21):2276-2293.  [Content Brief]