| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Haspin and DYRK2 (dual-specificity tyrosine-regulated kinase 2). LDN-192960 hydrochloride is a dual inhibitor of haspin and DYRK2 with IC₅0 values of 10 nM and 48 nM, respectively. It shows selectivity over TRKB, CLK1, DYRK1A, DYRK3, ROS, HIPK1, HIPK2, PIM-1, and PIM-2 kinases (IC₅0s = 720-91,000 nM).
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| ln Vitro |
Only five types of inhibition (IC50<1 μM) are effectively suppressed by LDN-192960 hydrochloride (10 μM). These are CLK1 (IC 50 = 0.21 μM), DYRK1A (IC50 = 0.10 μM), DYRK2 (IC50 = 2 nM), DYRK3 (IC50 = 19 nM), and PIM1 (IC50 = 0.72 μM) [1]. With an EC50 of 1.17 μM, LDN-0192960 hydrochloride (0-5 μM; 2 hours) reduces p-Thr3H3 levels in Haspin-overexpressing HeLa cells, exhibiting the characteristic Haspin suppressor phenotype[2]. By lowering p-Thr3H3 levels in mitotically synchronized HeLa cells, LDN-0192960 hydrochloride (0-1 μM; nuke for 1 hour in the presence of nocodazole and MG132) exhibits the characteristic Haspin inhibitory phenotype (EC50 0.02 μM) [2].
LDN-192960 hydrochloride inhibits haspin with an IC₅0 of 10 nM and DYRK2 with an IC₅0 of 48 nM. It is selective for haspin and DYRK2 over a panel of other kinases (IC₅0s = 720-91,000 nM). The compound is used for studying cell cycle regulation and kinase signaling. |
| ln Vivo |
In vivo, LDN-192960 hydrochloride would be expected to modulate haspin and DYRK2 activity, affecting cell cycle progression and cellular signaling. The compound could be used to study the roles of haspin in mitosis and DYRK2 in cell cycle regulation and cancer. Efficacy would be assessed in appropriate disease models.
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| Enzyme Assay |
Kinase activity assays are performed using recombinant haspin or DYRK2 enzymes. The kinase is incubated with ATP and a peptide substrate in the presence of serial dilutions of test compound. Phosphorylation of the substrate is detected by fluorescence, luminescence, or radiometric methods. IC₅0 values are calculated from dose-response curves.
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| Cell Assay |
Cells (e.g., cancer cell lines) are treated with LDN-192960 hydrochloride at various concentrations. Haspin and DYRK2 substrate phosphorylation (e.g., histone H3T3 phosphorylation for haspin) is assessed by Western blotting using phospho-specific antibodies. Cell cycle progression is evaluated by flow cytometry. Cell viability and proliferation are assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
Mice bearing tumor xenografts or other disease models are administered LDN-192960 hydrochloride via appropriate routes. Target engagement and pathway modulation are assessed by Western blotting of tumor tissues. Efficacy is determined by tumor growth inhibition or disease outcome measures.
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| ADME/Pharmacokinetics |
LDN-192960 hydrochloride has a molecular weight of 401.35 g/mol and formula C1₈H22Cl2N2O2S. Standard PK parameters (half-life, Cmax, AUC, clearance, volume of distribution) would be determined in rodent studies. The compound is formulated in suitable vehicles (e.g., DMSO) for in vivo administration.
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| Toxicity/Toxicokinetics |
Toxicology data for LDN-192960 hydrochloride are not publicly available. Standard preclinical safety assessment would include cytotoxicity screening, hERG channel inhibition testing, and repeat-dose toxicology studies in rodents. Given the roles of haspin and DYRK2 in cell cycle regulation, potential on-target toxicities would be evaluated.
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| References | |
| Additional Infomation |
LDN-192960 hydrochloride is a research compound for studying kinase biology and cell cycle regulation. It is not clinically approved. The compound's selectivity for haspin and DYRK2 over other kinases makes it a valuable tool for dissecting the distinct roles of these kinases in mitosis, cell cycle progression, and cancer.
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| Molecular Formula |
C18H22CL2N2O2S
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|---|---|
| Molecular Weight |
401.3505
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| Exact Mass |
400.077
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| CAS # |
2309172-48-1
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| Related CAS # |
LDN-192960;184582-62-5
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| PubChem CID |
91885401
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
343
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].Cl[H].S(C([H])([H])C([H])([H])C([H])([H])N([H])[H])C1C2C([H])=C(C([H])=C([H])C=2N=C2C([H])=C([H])C(=C([H])C=12)OC([H])([H])[H])OC([H])([H])[H]
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| InChi Key |
FNHCUCJBABESJB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H20N2O2S.2ClH/c1-21-12-4-6-16-14(10-12)18(23-9-3-8-19)15-11-13(22-2)5-7-17(15)20-16;;/h4-7,10-11H,3,8-9,19H2,1-2H3;2*1H
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| Chemical Name |
3-(2,7-dimethoxyacridin-9-yl)sulfanylpropan-1-amine;dihydrochloride
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~7.14 mg/mL (~17.79 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.71 mg/mL (1.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 7.1 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. Solubility in Formulation 2: 0.71 mg/mL (1.77 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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 | 2.4916 mL | 12.4580 mL | 24.9159 mL | |
| 5 mM | 0.4983 mL | 2.4916 mL | 4.9832 mL | |
| 10 mM | 0.2492 mL | 1.2458 mL | 2.4916 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.
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