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LSD1-IN-46 is a potent and orally active inhibitor of lysine-specific demethylase 1 (LSD1) with an IC50 value of 0.082 μM. It effectively blocks β-catenin-mediated transcriptional programs, thereby inhibiting the stemness of gastric cancer cells. LSD1-IN-46 exhibits significant antitumor activity and can be utilized in gastric cancer research.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | LSD1-IN-46 is a potent and orally active inhibitor of lysine-specific demethylase 1 (LSD1) with an IC50 value of 0.082 μM. It effectively blocks β-catenin-mediated transcriptional programs, thereby inhibiting the stemness of gastric cancer cells. LSD1-IN-46 exhibits significant antitumor activity and can be utilized in gastric cancer research. |
| Targets&IC50 | LSD1:0.082 μM |
| In vitro | LSD1-IN-46 (Compound X-1) at concentrations of 0.5-2 μM over 5 days increases H3K4me1/2 levels in MKN-45 cells; this effect is absent in LSD1 knockout cells. Additionally, LSD1-IN-46 inhibits the self-renewal, sphere formation, and colony-forming abilities of MKN-45 cells, while downregulating the expression of β-catenin, c-Myc, and stem cell markers OCT4, NANOG, and SOX2. |
| In vivo | LSD1-IN-46 (Compound X-1), administered orally by gavage at a dosage of 10-20 mg/kg once daily for 11 consecutive days, results in a reduction of both the size and weight of tumors in BALB/c nude mice that have been subcutaneously injected with MFC gastric cancer cells. |
| Molecular Weight | 351.49 |
| Formula | C22H29N3O |
| Cas No. | 2982716-97-0 |
| Smiles | O1C=2C=CC=CC2N(C=3C=CC=CC13)CCCN4CCC(N(C)C)CC4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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