LDN-192960
Based on 2 publication(s) in Google Scholar
LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
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- Reinheit: 99.58%
- CAS. Nr.: 184582-62-5
- Formel: C18H20N2O2S
- Molecular Weight:328.43
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) LDN-192960
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Biologische Aktivität
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DYRK1 |
DYRK2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | GI50 |
3.032 μM
Compound: LDN192960
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Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay
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[PMID: 38033250] |
| DU-145 | GI50 |
14.49 μM
Compound: LDN192960
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Antiproliferative activity against human DU-145 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human DU-145 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay
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[PMID: 38033250] |
| HT-22 | IC50 |
14.5 μM
Compound: 46; LDN192960
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Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
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[PMID: 36876904] |
| PC-3 | GI50 |
12.59 μM
Compound: LDN192960
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Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay
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[PMID: 38033250] |
LDN-192960 (10 μM) is selective and inhibits ten of the other kinases by ≥90%, with only five being potently inhibited (IC50<1 μM), including CLK1 (IC50=0.21 μM), DYRK1A (IC50= 0.10 μM), DYRK2 (IC50=2 nM), DYRK3 (IC50=19 nM) and PIM1 (IC50=0.72 μM)[1].LDN-0192960 (0-5 μM; 2 hours) demonstrates that the classical Haspin inhibition phenotype by reducing levels of p-Thr3H3 in HeLa cells overexpressing Haspin with an EC50 of 1.17 μM[2].LDN-0192960 (0-1 μM; 1 hour incubation in the presence of nocodazole and MG132) demonstrates the classical Haspin inhibition phenotype by reducing levels of p-Thr3H3 in HeLa cells synchronized in mitosis with an EC50 of 0.02 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 184582-62-5
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Appearance Solid
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Molecular Weight 328.43
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Formel C18H20N2O2S
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Color Yellow to orange
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SMILES
NCCCSC1=C(C=C(OC)C=C2)C2=NC3=CC=C(OC)C=C31
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845 -
Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (76.12 mM; Need ultrasonic; 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. 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. 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)
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Cuny GD, et al. Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3491-4. [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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0448 mL | 15.2239 mL | 30.4479 mL | 76.1197 mL |
| 5 mM | 0.6090 mL | 3.0448 mL | 6.0896 mL | 15.2239 mL | |
| 10 mM | 0.3045 mL | 1.5224 mL | 3.0448 mL | 7.6120 mL | |
| 15 mM | 0.2030 mL | 1.0149 mL | 2.0299 mL | 5.0746 mL | |
| 20 mM | 0.1522 mL | 0.7612 mL | 1.5224 mL | 3.8060 mL | |
| 25 mM | 0.1218 mL | 0.6090 mL | 1.2179 mL | 3.0448 mL | |
| 30 mM | 0.1015 mL | 0.5075 mL | 1.0149 mL | 2.5373 mL | |
| 40 mM | 0.0761 mL | 0.3806 mL | 0.7612 mL | 1.9030 mL | |
| 50 mM | 0.0609 mL | 0.3045 mL | 0.6090 mL | 1.5224 mL | |
| 60 mM | 0.0507 mL | 0.2537 mL | 0.5075 mL | 1.2687 mL |
LDN-192960 Related Classifications
HY-13455 Related Classifications
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