LSD1-IN-14
LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells.
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- CAS. Nr.: 2698340-11-1
- Formel: C21H24FN5
- Molecular Weight:365.45
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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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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 0.89 μM (LSD1)[1]
In Vitro
LSD1-IN-14 (compound x43) (0-20 μM; 72 hours) has a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively[1].
LSD1-IN-14 (0-3 μM ;72 hours) significantly upregulates the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner[1].
LSD1-IN-14 (0-3 μM;72 hours) induces the apoptosis of 53.6% of A549 cells in a dose-dependent manner[1].
LSD1-IN-14 (1 mM; 60 minutes) has excellent stability in human liver microsomes and weak CYP inhibition, with T1/2 of 103.3 min and Clint(mic) of 13.4 μL/min/mg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 and THP-1[1]
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Concentration:0-20 μM
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Incubation Time:72 hours
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Result:Showed a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively.
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Cell Line:A549 cells[1]
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Concentration:0, 0.3, 1 and 3 μM
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Incubation Time:72 hours
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Result:Significantly upregulated the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner.
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Cell Line:A549 cells[1]
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Concentration:0, 0.3, 1 and 3 μM
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Incubation Time:72 hours
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Result:Induced the apoptosis of 53.6% of cells in a dose-dependent manner.
In Vivo
Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats[1].
| IV (2 mg/kg) | IG (10 mg/kg) | ||
| C0 (ng/mL) | 575 | Cmax (ng/mL) | 41.1 |
| T1/2 (h) | 1.0 | T1/2 (h) | 2.8 |
| Vdss (L/kg) | 6.6 | Tmax (h) | 0.8 |
| Cl (mL/min/kg) | 156 | AUC0-t (ng.h/mL) | 126 |
| AUC0-t (ng.h/mL) | 211 | AUC0-∞ (ng.h/mL) | 152 |
| AUC0-∞ (ng.h/mL) | 214 | Bioacailability (%) | 11.9 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[1]
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Dosage:2 mg/kg for i.v., 10 mg/kg for i.g.
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Administration:i.v. and i.g, single
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Result:Showed an acceptable half-life and oral bioavailability.
Chemical Information
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CAS. Nr. 2698340-11-1
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Molecular Weight 365.45
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Formel C21H24FN5
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SMILES
CN(CCN(C1=CC=C(C=C1)NC2=NC=C(C=N2)C3=CC=C(C=C3)F)C)C
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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-14 Related Classifications
HY-145861 Related Classifications
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