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LDN-192960 hydrochloride

Names

[ CAS No. ]:
2309172-48-1

[ Name ]:
LDN-192960 hydrochloride

Biological Activity

[Description]:

LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> DYRK
Signaling Pathways >> Cell Cycle/DNA Damage >> Haspin Kinase

[Target]

IC50: 10 nM (Haspin); 48 nM (DYRK2)[1]


[In Vitro]

LDN-192960 hydrochloride (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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C18H22Cl2N2O2S

[ Molecular Weight ]:
401.35


Related Compounds