LDN-192960

Catalog No.S3406

For research use only.

LDN-192960 (Compd 1) is a potent inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50 of 10 nM and 48 nM, respectively.

LDN-192960 Chemical Structure

CAS No. 184582-62-5

Selleck's LDN-192960 has been cited by 1 Publication

Purity & Quality Control

Choose Selective Haspin Kinase Inhibitors

Biological Activity

Description LDN-192960 (Compd 1) is a potent inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50 of 10 nM and 48 nM, respectively.
Targets
Haspin [1]
(Cell-free assay)
DYRK2 [1]
(Cell-free assay)
10 nM 48 nM
In vitro

LDN-192960 (Compd 1) exerts functional inhibitory activity against Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM.[1]

Protocol (from reference)

Kinase Assay:

[1]

  • In vitro TR-FRET haspin assay:

    Kinase reactions were performed in 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM DTT, 0.01% Brij-35 using Proxiplate 384 Plus white assay plates. MBP-Haspin at 0.17 nM (0.05 nM enzyme final) and 0.33 M biotinylated H3(1-21) peptide (0.1 M peptide final, at the Km) in a volume of 3 μL kinase buffer were added to 2 μL solutions of compound. The kinase reaction was initiated by addition of 5 μL of 400 μM ATP per reaction (200 M ATP final, near Km). The reaction was incubated for 10 minutes at room temperature. Reaction was terminated by addition of 10 μL 50 mM EDTA, 2 nM Europium labeled anti-Histone H3T3ph antibody, 40 nM Streptavidin-APC. After a two hour incubation at room temperature, TR-FRET measurements were performed.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 328.43
Formula

C18H20N2O2S

CAS No. 184582-62-5
Storage 3 years -20°C powder
2 years -80°C in solvent

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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