| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C27H25Cl2F2N3O |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
LSD1-IN-26 is a potent LSD1 inhibitor, with an IC50 of 25.3 nM. It also inhibits MAO-A (IC50 1234.57 nM) and MAO-B (IC50 3819.27 nM), and significantly induces apoptosis in MGC-803 cells. It can be used in gastric cancer research[1]. It has a molecular formula of C27H25Cl2F2N3O and a molecular weight of 516.41 g/mol.
Physical & Chemical Properties
| CAS Number | 3041141-72-1 |
|---|---|
| Molecular Formula | C27H25Cl2F2N3O |
| Molecular Weight | 516.41 g/mol |
| 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 |
| Target | LSD1, MAO-A, MAO-B, Bcl-2, cIAP-1, Caspase-3, Caspase-9 |
| Signaling Pathway | Epigenetics; Neuronal Signaling; Apoptosis |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
|
LSD1 25.3 ± 1.4 nM (IC50) |
MAO-A 1234.57 nM (IC50) |
MAO-B 3819.27 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
LSD1-IN-26 is highly potent against MGC-803, KYSE450 and HCT-116 cells (IC50 values of 14.3±1.18, 22.8±1.45 and 16.3±2.22 μM, respectively), outperforming both GSK-LSD1 and GSK-2879552, whose IC50 values are above 64 μM (> 64 μM)[1]. At 0-24 μM for 48 h, LSD1-IN-26 causes H3K4 Me1/2 and H3K9 Me2/3 to accumulate and Bcl-2 and c-IAP1 to decrease[1]. Under the same conditions (0-24 μM, 48 h), it induces apoptosis and differentiation and inhibits migration and cell stemness[1].
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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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