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ML385

Cat. No. M8692

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ML385 Structure
Synonym:

ML-385

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 55  USD55 In stock
1mg USD 25  USD25 In stock
5mg USD 50  USD50 In stock
10mg USD 80  USD80 In stock
25mg USD 165  USD165 In stock
50mg USD 260  USD260 In stock
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Biological Activity

ML385 inihbits the activity of the Nrf2 transcription factor by binding to Neh1, a NC-bZIP domain that allows Nrf2 to heterodimerize with small Maf proteins, blocking NRF2 transcriptional activity. Much research has been done on activating Nrf2 because it induces cytoprotective antioxidant genes. However, some cancer cells may use Nrf2 similarly for their survival. Nrf2 is overexpressed in certain cancers such as non-small cell lung cancer (NSCLC) often due to loss of function mutations in KEAP1, which targets Nrf2 for proteasomal degradation. ML385 was found to have anti-tumor activity with specificity and selectivity for NSCLC cells with KEAP1 mutations.

Product Citations
Customer Product Validations & Biological Datas
Source Front Oncol (2021). Figure 4. ML-385 (Abmole Bioscience, Houston, TX, USA)
Method Cell Migration and Cell Invasion Assays
Cell Lines Murine BC cell line 4T1 cells
Concentrations 0, 5, 10 µM
Incubation Time -
Results We found that ML-385 treatment significantly attenuated NRF2, p-NRF2 expression (Figure 4A) and NRF2-responsive gene levels (Figure 4B) in DPP-4i-treated BC cells. Notably, DPP-4i-driven BC cell migration and invasion were significantly abrogated by ML-385 treatment with a dose-dependent manner (Figures 4C, D). Furthermore, DPP-4i–driven metastasis-associated gene levels were significantly attenuated after ML-385 treatment in BC cells (Figure 4E). These data indicate that NRF2 inhibition reverses DPP-4i–driven BC metastases in vitro.
Protocol (for reference only)
Cell Experiment
Cell lines IPEC-J2 cells
Preparation method IPEC-J2 cells were cultured in DMEM/F12 supplemented with 5% FBS, 5% PS, 1% ITS, and 5 ng/mL EGF in a 5% CO2 atmosphere at 37°C. Cells were treated with PBS or different pathway inhibitors (5 μM ML385, 10 μM LY294002, 1 μM Mdivi-1) for 1 h, and then treated with HT (50 μM) for 9 h, followed by DQ (75 μM) for 6 h. Then, cells were collected for ELISA, western blot, and transmission electron microscopy (TEM) after washed twice by cold PBS.
Concentrations 5 μM
Incubation time 1 h
Animal Experiment
Animal models Female nude mice
Formulation DMSO
Dosages 30 mg/kg
Administration Intraperitoneal injection
Chemical Information
Molecular Weight 511.59
Formula C29H25N3O4S
CAS Number 846557-71-9
Solubility (25°C) DMSO ≥ 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Anju Singh, et al. ACS Chem Biol. Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors

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  Catalog
Abmole Inhibitor Catalog




Keywords: ML385, ML-385 supplier, Keap1-Nrf2, inhibitors, activators

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