| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
| Targets |
IC50: 55 nM (haspin kinase) IC50: 9.9 μM (DYRK2)[1]
LDN-209929 dihydrochloride selectively targets haspin kinase (also known as haploid germ cell-specific nuclear protein kinase), a serine/threonine kinase essential for proper mitotic chromosome segregation and cell division. It exhibits high selectivity for haspin over DYRK2, with 180-fold selectivity (IC50=55 nM vs. 9.9 μM). By inhibiting haspin, this compound is used to study its role in mitosis and cell cycle regulation. |
|---|---|
| ln Vitro |
Serine/threonine kinase Haspin, also known as Haploid Germ Cell-Specific Nuclear Protein Kinase, is expressed in a number of different tissues, including the testis, bone marrow, thymus, and spleen. Furthermore, haspin is crucial during mitosis, where it phosphorylates histone H3 at Thr-3 (H3T3) in G2/early prophase, reaches its peak in prometaphase/metaphase, and then starts to decline in anaphase[1]. DYRKs are ePKs that are a part of the CMGC family. They are further classified into two classes: class 2 kinases (DYRK2, 3, and 4) and class 1 kinases (DYRK1A and 1B). During synthesis, a critical activation loop tyrosine is autophosphorylated, which is necessary for DYRK activity[1].
In vitro, LDN-209929 dihydrochloride demonstrates potent inhibition of haspin kinase with an IC50 of 55 nM. It shows 180-fold selectivity over DYRK2 (IC50=9.9 μM), making it a highly specific tool for studying haspin function. As an optimized analogue of LDN-192960, it was specifically designed to overcome the off-target inhibition of DYRK2 that limited earlier haspin inhibitors. Its high potency and selectivity make it suitable for studying haspin-dependent phosphorylation events in cell cycle and mitosis research. |
| ln Vivo |
In vivo data for LDN-209929 dihydrochloride is not extensively reported in publicly available sources. As a potent and selective haspin kinase inhibitor, the compound has potential applications in animal models to study the role of haspin in mitosis, chromosome segregation, and cell division. However, specific published in vivo efficacy studies are not detailed in the current literature. LDN-209929 dihydrochloride is primarily used as a research tool for studying cell cycle regulation and mitotic processes.
|
| Enzyme Assay |
The in vitro haspin kinase inhibition assay for LDN-209929 dihydrochloride uses recombinant haspin kinase and a peptide substrate. Kinase activity is measured using radioactive or luminescent detection methods, and IC50 values are calculated from dose-response curves. Selectivity profiling against DYRK2 is performed using similar assay formats to confirm the 180-fold selectivity. The compound is typically tested at concentrations ranging from nanomolar to micromolar to determine its inhibitory potency.
|
| Cell Assay |
Cellular assays for LDN-209929 dihydrochloride are conducted in various cell lines to study its effects on mitosis and chromosome segregation. Cells are treated with varying concentrations of the compound, and the effects on cell cycle progression are analyzed by flow cytometry. Haspin inhibition is confirmed by assessing the phosphorylation status of known haspin substrates such as histone H3T3ph. Cell viability and proliferation are measured using standard assays such as MTT. The compound's specificity is validated by comparing its effects with other haspin inhibitors.
|
| Animal Protocol |
In vivo studies for LDN-209929 dihydrochloride would typically involve animal models to study the role of haspin in mitosis and cell division. The compound would be administered via intraperitoneal or oral routes at doses determined by pharmacokinetic studies. Efficacy would be assessed by analyzing cell cycle progression and chromosome segregation in tissues. However, specific published in vivo protocols for LDN-209929 dihydrochloride are not available in the current literature. The compound is currently used as a research tool for studying haspin function.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for LDN-209929 dihydrochloride is not extensively reported in publicly available sources. The compound has a molecular weight of 405.77 g/mol and a molecular formula of C17H19Cl3N2OS. It is supplied as a dihydrochloride salt for enhanced solubility and handling. The compound is soluble in DMSO. Storage conditions: powder at -20°C for 3 years or 4°C for 2 years. Detailed PK parameters such as half-life and bioavailability are not available in the current literature.
|
| Toxicity/Toxicokinetics |
Toxicity data for LDN-209929 dihydrochloride is limited in publicly available sources. As with all research compounds, LDN-209929 dihydrochloride is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment. The compound's high selectivity for haspin over DYRK2 suggests a favorable off-target profile.
|
| References | |
| Additional Infomation |
LDN-209929 dihydrochloride is a potent and selective haspin kinase inhibitor (IC50=55 nM) with 180-fold selectivity over DYRK2 (IC50=9.9 μM). It is an optimized analogue of LDN-192960, engineered to address substantial off-target DYRK2 inhibition. Haspin is a serine/threonine kinase critical for mitotic chromosome segregation. The dihydrochloride salt enhances aqueous solubility for in vitro handling. LDN-209929 dihydrochloride is a valuable tool for studying cell cycle regulation, mitosis, and haspin-dependent phosphorylation events. It has a molecular formula of C17H19Cl3N2OS and a molecular weight of 405.77 g/mol.
|
| Molecular Formula |
C17H19CL3N2OS
|
|---|---|
| Molecular Weight |
405.769560098648
|
| Exact Mass |
404.028
|
| CAS # |
1784281-97-5
|
| PubChem CID |
90488975
|
| Appearance |
Yellow to orange solid powder
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
24
|
| Complexity |
360
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C=CC2=C(C=1)C(=C1C=C(C=CC1=N2)OC)SCCCN.Cl.Cl
|
| InChi Key |
WOCCOXNODBCCGK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H17ClN2OS.2ClH/c1-21-12-4-6-16-14(10-12)17(22-8-2-7-19)13-9-11(18)3-5-15(13)20-16;;/h3-6,9-10H,2,7-8,19H2,1H3;2*1H
|
| Chemical Name |
3-(2-chloro-7-methoxyacridin-9-yl)sulfanylpropan-1-amine;dihydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : 33.33 mg/mL (82.14 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4645 mL | 12.3223 mL | 24.6445 mL | |
| 5 mM | 0.4929 mL | 2.4645 mL | 4.9289 mL | |
| 10 mM | 0.2464 mL | 1.2322 mL | 2.4645 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
