LDN-192960

Catalog No.S3406 Batch:S340601

Technical Data

Formula	C₁₈H₂₀N₂O₂S
Molecular Weight	328.43	CAS No.	184582-62-5
Solubility (25°C)*	In vitro	Water	66 mg/mL (200.95 mM)
		DMSO	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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.

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.

References

[1] Gregory D Cuny, et al. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3491-4.

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

Kinase DYRK2 acts as a regulator of autophagy and an indicator of favorable prognosis in gastric carcinoma [ Colloids Surf B Biointerfaces, 2022, 209(Pt 1):112182]	PubMed: 34749023

Kinase DYRK2 acts as a regulator of autophagy and an indicator of favorable prognosis in gastric carcinoma [ Colloids Surf B Biointerfaces, 2022, 209(Pt 1):112182]

PubMed: 34749023

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