Conditionnement : 5mg
Synonyms:
| Description | ML385 is an NRF2 inhibitor (IC50=1.9 μM) with novelty and specificity. ML385 has anti-inflammatory activity by modulating anti-oxidative stress through the inhibition of NRF2. ML385 also exhibits anti-tumor activity. |
| Targets & IC50 | Nrf2:1.9 μM |
| In vitro | Method: Human lung cancer cells A549 were treated with ML385 (0.25-5 μM) for 12-72 h. The expression levels of target genes were detected by RT-qPCR. Result: ML385 dose-dependently and time-dependently decreased the transcriptional activity of NRF2. [1] Method: Human lung cancer cells EBC1 were treated with ML385 (1-25 μM) for 48 h, and the expression levels of target proteins were detected by Western Blot. Result: NRF2 expression was inhibited by treatment with 5 μM ML385. When the concentration of ML385 was increased above 5 μM, the NRF2 protein level was restored. [2] |
| In vivo | Method: To detect anti-tumor activity in vivo, ML385 (30 mg/kg) and carboplatin (5 mg/kg) were intraperitoneally injected into athymic nude mice harboring human lung cancer tumors A549 or H460 five times a week for three weeks. Result: Treatment with ML385 in combination with carboplatin showed a significant reduction in tumor growth. Although treatment with a single agent resulted in a reduction in tumor growth, the magnitude of these effects was variable between cell lines and did not reach statistical significance. [1] Method: To investigate whether Nrf2 modulates acute liver failure (ACLF) through iron death, ML385 (30 mg/kg) was injected intraperitoneally four times per week for four weeks into BALB/c mice constructed in the ACLF model. Result: More severe histopathological lesions were observed in the ML385 group compared to the ACLF group. lipid peroxidation and liver injury were exacerbated by the Nrf2 inhibitor, ML385. [3] |
| Cell Research | cells are treated with ML385 for 36 h. An equal amount of CellTiter-Blue reagent is added to the wells and the fluorescence is measured after 30 min. The CellTiter-Blue reagent is discarded and the Caspase-Glo (100 μL) reagent is added to the cells and incubated at 37°C for an additional 60-90 min. The resulting luminescence is recorded and the caspase activity is normalized to cell number |
| Animal Research | Mice tumor xenografts are administered intraperitoneally ML385 (30 mg/kg). |
| Molecular Weight | 511.59 |
| Formula | C29H25N3O4S |
| Cas No. | 846557-71-9 |
| Smiles | O=C(NC1=NC(C2=CC=C(N(C(C3=C(C)C=CC=C3)=O)CC4)C4=C2)=C(C)S1)CC5=CC(OCO6)=C6C=C5 |
| Relative Density. | 1.374 g/cm3 (Predicted) |
| Storage | Keep away from direct sunlight Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50.00 mg/mL (97.73 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.00 mg/mL (5.86 mM), Suspension. 50% PEG300+50% Saline: 5.00 mg/mL (9.77 mM), Suspension. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.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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