1. Epigenetics Neuronal Signaling Apoptosis
  2. Histone Demethylase Monoamine Oxidase Apoptosis Bcl-2 Family IAP Caspase
  3. LSD1-IN-26

LSD1-IN-26 (compound 12u) is a potent LSD1 inhibitor, with an IC50 of 25.3 nM. LSD1-IN-26 also inhibits MAO-A (IC50=1234.57 nM) and MAO-B (IC50=3819.27 nM). LSD1-IN-26 significantly induces apoptosis in MGC-803 cells. LSD1-IN-26 can be used for gastric cancer research.

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LSD1-IN-26 Chemical Structure

LSD1-IN-26 Chemical Structure

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Description

LSD1-IN-26 (compound 12u) is a potent LSD1 inhibitor, with an IC50 of 25.3 nM. LSD1-IN-26 also inhibits MAO-A (IC50=1234.57 nM) and MAO-B (IC50=3819.27 nM). LSD1-IN-26 significantly induces apoptosis in MGC-803 cells. LSD1-IN-26 can be used for gastric cancer research[1].

IC50 & Target

LSD1

25.3 ± 1.4 nM (IC50)

MAO-A

1234.57 nM (IC50)

MAO-B

3819.27 nM (IC50)

Bcl-2

 

cIAP-1

 

Caspase-3

 

Caspase-9

 

In Vitro

LSD1-IN-26 (compound 12u) shows the high potency against MGC-803, KYSE450 and HCT-116 cells with IC50 values of 14.3±1.18, 22.8±1.45 and 16.3±2.22 μM, respectively, which is more potent than that of GSK-LSD1 (HY-100546) (IC50 > 64 μM) and GSK-2879552 (HY-18632) (IC50 > 64 μM)[1].
LSD1-IN-26 (0-24 μM, 48 h) induces the accumulation of H3K4 Me1/2 and H3K9 Me2/3 and the decrease of Bcl-2 and c-IAP1[1].
LSD1-IN-26 (0-24 μM, 48 h) induces apoptosis and differentiation, and inhibits migration and cell stemness[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MGC-803 cells
Concentration: 0, 8, 16, 24 μM
Incubation Time: 48 h
Result: Effectively up-regulated the substrate proteins of LSD1, thereby significantly increasing the expression levels of mono-/bi-methylation of H3K4 and H3K9. Dose-dependently induced the decrease of expression levels of anti-apoptotic proteins Bcl-2 and c-IAP1, and the cleavage of apoptotic executive proteins Caspase3 and Caspase9.
Molecular Weight

516.41

Formula

C27H25Cl2F2N3O

SMILES

O=C(N1CCN(CC1)C2=CC(Cl)=C(C=C2)Cl)C3=CC=CC(CN[C@@H]4C[C@H]4C5=CC=C(C(F)=C5)F)=C3

Shipping

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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    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-26
Cat. No.:
HY-149978
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