Home Cell Cycle Haspin Kinase inhibitor - DYRK inhibitor LDN-192960 For research use only.

LDN-192960

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

LDN-192960 Chemical Structure

CAS: 184582-62-5

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

Purity & Quality Control

Batch: S340601 Water] 66 mg/mL] false] DMSO] Insoluble] false] Ethanol] Insoluble] false Purity: 99.56%
99.56

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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
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]
Kinase Assay 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.

Chemical Information & Solubility

Molecular Weight 328.43 Formula

C18H20N2O2S
CAS No. 184582-62-5 SDF --
Smiles COC1=CC2=C(SCCCN)C3=C(C=CC(=C3)OC)N=C2C=C1
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Water : 66 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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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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