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.
Storage Temp
Store at 2-8°C,Desiccated
Shipped In
Wet ice
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Product Description
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.
This compound belongs to the class of organic compounds known as acridines. These are organic compounds containing the acridine moiety, a linear tricyclic heterocycle which consists of two benzene rings joined by a pyridine ring.
External Descriptors
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1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
