Home Cell Cycle Haspin Kinase inhibitor LDN-192960

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LDN-192960 Haspin Kinase inhibitor

Cat.No.S3406

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 Haspin Kinase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 328.43

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Quality Control

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

Solubility

In vitro
Batch:

Water : 66 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 328.43 Formula

C18H20N2O2S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 184582-62-5 -- Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC2=C(SCCCN)C3=C(C=CC(=C3)OC)N=C2C=C1

Mechanism of Action

Targets/IC50/Ki
Haspin
(Cell-free assay)
10 nM
DYRK2
(Cell-free assay)
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.
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.
References

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