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Keap1-Nrf2-IN-4, a powerful neddylation inhibitor, demonstrates significant anti-proliferation activity against MGC-803 cells (IC50 = 2.55 μM), effectively impeding their migration and inducing apoptosis. Additionally, it effectively inhibits tumor growth while exhibiting minimal toxicity [1].
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 10-14 weeks | 10-14 weeks | |
| 50 mg | $1,980 | 10-14 weeks | 10-14 weeks | |
| 100 mg | $2,500 | 10-14 weeks | 10-14 weeks |
| Description | Keap1-Nrf2-IN-4, a powerful neddylation inhibitor, demonstrates significant anti-proliferation activity against MGC-803 cells (IC50 = 2.55 μM), effectively impeding their migration and inducing apoptosis. Additionally, it effectively inhibits tumor growth while exhibiting minimal toxicity [1]. |
| In vitro | Keap1-Nrf2-IN-4 (compound 4g) shows significant anti-proliferative effects with IC50 values of 2.55, 3.88, 3.74, and 2.89 μM in MGC-803, MCF-7, A549, and HepG-2 cell lines, respectively, after 72 hours. It inhibits the neddylation of cullin1, cullin3, and cullin5, obstructs the migratory ability of MGC-803 cells without causing cell cycle arrest, and induces apoptosis in MGC-803 and HGC-27 cells in a concentration- and time-dependent manner when applied for 24 and 48 hours, indicating its potential as a cancer therapeutic. |
| In vivo | Keap1-Nrf2-IN-4, administered orally at dosages of 50 and 100 mg/kg daily for a duration of 21 days, demonstrated effective antitumor activity in a xenograft model utilizing 5-6 weeks old, 18-20 g NOD SCID mice, without manifesting any evident adverse effects [1]. |
| Molecular Weight | 390.56 |
| Formula | C26H34N2O |
| Smiles | #N/A |
| 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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