LDN-209929 dihydrochloride
Based on 1 Customer Validation
LDN-209929 dihydrochloride is a potent and selective haspin kinase inhibitor (IC50=55 nM) with180-fold selectivity verses DYRK2 (IC50=9.9 μM). LDN-209929 is a optimized analogue of LDN-192960 (HY-13455).
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- Reinheit: 98.33%
- CAS. Nr.: 1784281-97-5
- Formel: C17H19Cl3N2OS
- Molecular Weight:405.77
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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DYRK2 |
Haspin: Haploid Germ Cell-Specific Nuclear Protein Kinase, is a serine/threonine kinase expressed in a variety of tissues (e.g., testis, bone marrow, thymus, and spleen). Haspin also plays an important role in mitosis, where it phosphorylates histone H3 at Thr-3 (H3T3) in G2/early prophase, becomes maximal during prometaphase/metaphase and then diminishes during anaphase[1]. DYRKs belong to the CMGC family of ePKs and can be further divided into class 1 kinases DYRK1A and 1B, and class 2 kinases DYRK2, 3, and 4. The activity of DYRKs depends upon autophosphorylation of an essential activation loop tyrosine during synthesis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1784281-97-5
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Appearance Solid
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Molecular Weight 405.77
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Formel C17H19Cl3N2OS
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Color Yellow to orange
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SMILES
NCCCSC1=C(C=C(Cl)C=C2)C2=NC3=CC=C(OC)C=C31.[H]Cl.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 33.33 mg/mL (82.14 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Gregory D Cuny, et al. Structure-activity Relationship Study of Acridine Analogs as Haspin and DYRK2 Kinase Inhibitors. Bioorg Med Chem Lett [Content Brief]
[2]. Katrin Kestav, et al. Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin. Curr Med Chem. 2017;24(21):2276-2293. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4645 mL | 12.3223 mL | 24.6445 mL | 61.6113 mL |
| 5 mM | 0.4929 mL | 2.4645 mL | 4.9289 mL | 12.3223 mL | |
| 10 mM | 0.2464 mL | 1.2322 mL | 2.4645 mL | 6.1611 mL | |
| 15 mM | 0.1643 mL | 0.8215 mL | 1.6430 mL | 4.1074 mL | |
| 20 mM | 0.1232 mL | 0.6161 mL | 1.2322 mL | 3.0806 mL | |
| 25 mM | 0.0986 mL | 0.4929 mL | 0.9858 mL | 2.4645 mL | |
| 30 mM | 0.0821 mL | 0.4107 mL | 0.8215 mL | 2.0537 mL | |
| 40 mM | 0.0616 mL | 0.3081 mL | 0.6161 mL | 1.5403 mL | |
| 50 mM | 0.0493 mL | 0.2464 mL | 0.4929 mL | 1.2322 mL | |
| 60 mM | 0.0411 mL | 0.2054 mL | 0.4107 mL | 1.0269 mL | |
| 80 mM | 0.0308 mL | 0.1540 mL | 0.3081 mL | 0.7701 mL |
LDN-209929 dihydrochloride Related Classifications
HY-110320 Related Classifications
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