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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- CAS. Nr.: 3041141-72-1
- Formel: C27H25Cl2F2N3O
- Molecular Weight:516.41
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
Beschreibung
IC50 & Target
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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 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
16.3 μM
Compound: 12u
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Antiproliferative activity against human HCT-116 cells incubated for 48 hrs measured by MTT assay
Antiproliferative activity against human HCT-116 cells incubated for 48 hrs measured by MTT assay
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[PMID: 36881982] |
| KYSE-450 | IC50 |
22.8 μM
Compound: 12u
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Antiproliferative activity against human KYSE-450 cells incubated for 48 hrs measured by MTT assay
Antiproliferative activity against human KYSE-450 cells incubated for 48 hrs measured by MTT assay
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[PMID: 36881982] |
| MGC-803 | IC50 |
14.3 μM
Compound: 12u
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Antiproliferative activity against human MGC-803 cells incubated for 48 hrs measured by MTT assay
Antiproliferative activity against human MGC-803 cells incubated for 48 hrs measured by MTT assay
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[PMID: 36881982] |
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.
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Cell Line:MGC-803 cells
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Concentration:0, 8, 16, 24 μM
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Incubation Time:48 h
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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.
Chemical Information
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CAS. Nr. 3041141-72-1
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Molecular Weight 516.41
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Formel C27H25Cl2F2N3O
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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
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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-26 Related Classifications
HY-149978 Related Classifications
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