LSD1-IN-43
LSD1-IN-43 is a highly selective, reversible, orally active and brain-penetrant LSD1 inhibitor with an IC50 value of 0.8 μM. LSD1-IN-43 has low inhibitory activity against MAO-A and MAO-B, two homologs of LSD1. LSD1-IN-43 significantly inhibits Aβ aggregation and enhances Aβ-induced neuronal cell viability. LSD1-IN-43 can be used for the study of Alzheimer’s disease (AD).
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- 화학식: C23H23NO4
- 분자량:377.43
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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KDM1/LSD1 |
LSD1-IN-43 (10 μM) exhibits a highly selective and reversible inhibitory effect on LSD1, with minimal activity against MAO-A (7% inhibition) and MAO-B (4.9% inhibition)[1].
LSD1-IN-43 (25-100 μM) exhibits the low toxicity and effectively reduces Aβ1-42 generation levels in HT22 cells[1].
LSD1-IN-43 (10 μM) exhibits a significant inhibitory effect on Aβ1-42 aggregation, with a rate of 66.19%, which is much higher than 49.98% for Curcumin (HY-N0005)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LSD1-IN-43 (125-500 μM, 24-56 h) demonstrates a concentration-dependent ability to extend the lifespan and reduces paralysis onset in the CL4176 transgenic C. elegans model[1].
LSD1-IN-43 (40-80mg/kg, i.g.) restores the expression of H3K9me2 expression-a histone marker regulated by LSD1, while simultaneously improving learning, memory, and cognitive function deficits in this AD mouse mode [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:APP/PS1 Mice (5 weeks)[1]
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Dosage:40, 80 mg/kg
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Administration:Intragastric administration (i.g.)
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Result:Improved performance in the Morris Water Maze compared to the saline-treated APP/PS1 group.
Reduced escape latency and improved ability to locate the hidden platform compared to the saline-treated APP/PS1 group.
Increased correct alternations and better spatial recognition compared to the saline-treated APP/PS1 group.
Reduced the expression of neuroinflammatory markers (IBAI for microglia and GFAP for astrocytes) and inflammatory cytokines (IL-1β and TNF-α) in the hippocampal CA1 region of APP/PS1 mice compared to the saline-treated group.
Reduced Aβ 1-42 deposition in the hippocampus ,with high-dose treatment (80 mg/kg) showing a more pronounced reduction compared to the saline-treated APP/PS1 group.
Restored the expression of H3K9me2,which is a histone marker regulated by LSD1 compared to the saline-treated APP/PS1 group.
Increased inneuron density and compact arrangement, reduced inuclear pyknosis and cytoplasmic vacuolation compared to the saline-treated APP/PS1 group.
Chemical Information
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분자량 377.43
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화학식 C23H23NO4
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SMILES
C[C@@]12[C@](CC(C3=C2)=C(C)C(O3)=O)([H])C(CC4=CNC5=C4C(O)=CC=C5)C(CC1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LSD1-IN-43 Related Classifications
HY-176254 Related Classifications
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