LSD1-IN-48
LSD1-IN-48 is a tranylcypromine-pyrimidine derivative and selective LSD1 inhibitor with a human IC50 of 7.87 nM. LSD1-IN-48 increases H3K4me1/2 histone methylation levels. LSD1-IN-48 induces apoptosis, upregulates CD86, downregulates SOX2 and CD44, inhibits proliferation in cancer cells. LSD1-IN-48 can be used for the research of acute myeloid leukemia.
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- CAS No.: 3104325-26-7
- Formule: C18H18F2N6O3S
- Masse moléculaire:436.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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LSD1 7.87 nM (IC50) |
LSD1-IN-48 (7a) potently inhibits recombinant LSD1 with an IC50 of 7.87 nM and exhibits over 127-fold and 1270-fold selectivity for LSD1 over MAO-A and MAO-B, respectively[1].
LSD1-IN-48 inhibits the proliferation of MV-4-11, HL-60, and THP-1 acute myeloid leukemia cells with IC50 values of 0.36 μM, 0.48 μM, and 1.12 μM, respectively[1].
LSD1-IN-48 (10-100 μM) directly binds to LSD1 extracted from MV-4-11 cells, protecting the protein from alkaline protease hydrolysis in a dose-dependent manner[1].
LSD1-IN-48 shows metabolic stability in human liver microsomes with a half-life of 7.26 min and an intrinsic clearance of 172 mL/min/kg[1].
LSD1-IN-48 (0.5-2 μM; 2 days) increases H3K4me1 and H3K4me2 histone methylation levels in MV-4-11 cells in a dose-dependent manner[1].
LSD1-IN-48 (0.5-2 μM; 2 days) induces apoptosis in MV-4-11 cells in a dose-dependent manner and activates the caspase-mediated apoptotic pathway[1].
LSD1-IN-48 (0.5-2 μM; 4 days) dose-dependently upregulates the differentiation marker CD86 in MV-4-11 cells[1].
LSD1-IN-48 (0.5-2 μM; 96 h) dose-dependently reduces the levels of stem cell-associated proteins SOX2 and CD44 in MV-4-11 cells,[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:2 days
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Result:Dose-dependently increased the levels of H3K4me1 and H3K4me2; at 2 μM, H3K4me1 levels increased to ~4-fold and H3K4me2 levels increased to ~1.5-fold relative to the control.
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Cell Line:MV-4-11 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:2 days
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Result:Dose-dependently increased the total apoptosis rate; at 2 μM, the total apoptosis rate increased from 6.45% to 33.19%.
Dose-dependently increased the levels of cleaved caspase-3, cleaved caspase-7, and cleaved PARP.
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Cell Line:MV-4-11 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:4 days
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Result:Dose-dependently increased CD86 expression; at 2 μM, CD86 expression increased by 19.18% relative to the control.
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Cell Line:MV-4-11 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:96 h
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Result:Dose-dependently reduced the protein levels of SOX2 and CD44; at 2 μM, SOX2 levels were reduced to ~0.15-fold and CD44 levels were reduced to ~0.55-fold relative to the control.
| Species | Dose | Route | AUC0-∞ | AUC0-t | T1/2 | Cmax | CL |
|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 26.0 μg/L·h | 22.9 μg/L·h | 0.863 h | 57.2 μg/L | 38794 mL/h/kg |
Chemical Information
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CAS No. 3104325-26-7
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Masse moléculaire 436.44
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Formule C18H18F2N6O3S
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SMILES
O=S(C1=NC(N2C=C(CN[C@@H]3C[C@H]3C4=CC=C(F)C=C4F)N=N2)=CC(OC)=N1)(C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LSD1-IN-48 Related Classifications
HY-181781 Related Classifications
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