Description
| 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 |
METHODS: 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. RESULTS: ML385 dose-dependently and time-dependently decreased the transcriptional activity of NRF2. [1] METHODS: 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. RESULTS: 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 |
METHODS: 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. RESULTS: 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] METHODS: 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. RESULTS: 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 |
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 50 mg/mL (97.73 mM)
