1. Epigenetics Neuronal Signaling
  2. Histone Demethylase Amyloid-β
  3. 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 aggregation and enhances Aβ-induced neuronal cell viability. LSD1-IN-43 can be used for the study of Alzheimer’s disease (AD)[1].

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LSD1-IN-43 Chemical Structure

LSD1-IN-43 Chemical Structure

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Description

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 aggregation and enhances Aβ-induced neuronal cell viability. LSD1-IN-43 can be used for the study of Alzheimer’s disease (AD)[1].

In Vitro

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.

In Vivo

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.

Animal Model: APP/PS1 Mice (5 weeks)[1]
Dosage: 40, 80 mg/kg
Administration: Intragastric administration (i.g.)
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.
Molecular Weight

377.43

Formula

C23H23NO4

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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
LSD1-IN-43
Cat. No.:
HY-176254
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