LSD1-IN-25
LSD1-IN-25 (Compound 9j) is a potent, selective and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM). LSD1-IN-25 induces cancer cell apoptosis.
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- CAS. Nr.: 2911585-60-7
- Formel: C32H33ClN6O3S
- Molecular Weight:617.16
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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LSD1 46 nM (IC50) |
LSD1 30.3 nM (Ki) |
LSD1-IN-25 (Compound 9j; 0-20 μM; 72 h) inhibits solid tumor cell proliferation[1].
LSD1-IN-25 (1-4 μM; 24 h) induces the elevation of cellular H3K4me2 and inhibits the EMT process of H1650 cells[1].
LSD1-IN-25 (1-4 μM; 24 h) induces apoptosis and S arrest in H1650 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MGC-803, MGC-803LSD1-KO, SGC-7901, GES-1, MCF-7, H1650, A549, H460, PC-3 and EC-109
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Concentration:0-20 μM
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Incubation Time:72 h
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Result:Antiproliferative activity of LSD1-IN-25 (Compound 9j) on solid tumor cell lines[1]
Cell line Origin IC50 (μM) MGC-803 Gastric cancer 5.1 ± 0.7 MGC-803LSD1-KO Gastric cancer >20 SGC-7901 Gastric cancer 9.5 ± 2.1 GES-1 Normal gastric epithelial cell >20 MCF-7 Breast cancer 13.4 ± 2.4 H1650 Lung cancer 4.3 ± 0.9 A549 Lung cancer 7.9 ± 1.5 H460 Lung cancer 13.6 ± 4.2 PC-3 Prostate cancer 7.5 ± 1.1 EC-109 Esophageal cancer 15.2 ± 2.9
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Cell Line:H1650 cell
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Concentration:1, 2 and 4 μM
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Incubation Time:24 h
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Result:Induced the elevation of cellular H3K4me2. Elevated the expression of the epithelial marker E-cadherin, decreased the expression of the mesenchymal markers such as N-cadherin, slug and vimentin.
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Cell Line:H1650 cell
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Concentration:1, 2 and 4 μM
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Incubation Time:24 h
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Result:Induced an evident increase in cell apoptosis, with the percentage of apoptotic cells of 43.9% (1 μM), 44.5% (2 μM) and 45.7% (4 μM), respectively, in comparison with 12.7% of the control.
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Cell Line:H1650 cell
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Concentration:1, 2 and 4 μM
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Incubation Time:24 h
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Result:The percentage of cells in S phase were 29.97% 33.32%, 39.81%, 43.26% at concentrations of 0, 1 μM, 2 μM, 4 μM, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice, xenograft model of H1650 cells[1]
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Dosage:10 mg/kg and 20 mg/kg
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Administration:Oral, once daily for 21 days
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Result:Presented a remarkable reduction of average tumor weight by 41.5% and 64.0% at dosages of 10 and 20 mg/kg, respectively. Evidently prolonged the mice's survival.
Chemical Information
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CAS. Nr. 2911585-60-7
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Molecular Weight 617.16
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Formel C32H33ClN6O3S
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SMILES
ClC1=CC=CC(CN2C(N=C(SCCC)N=C3OC4=C(OC)C=C(CN[C@H]5C[C@@H]5C6=CC=CC=C6)C=C4OC)=C3N=N2)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
LSD1-IN-25 Related Classifications
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