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ML385

Cat. No. M8692
ML385 Structure
Synonym:

ML-385

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 60  USD60 In stock
5mg USD 50  USD50 In stock
10mg USD 90  USD90 In stock
25mg USD 190  USD190 In stock
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Quality Control & Documentation
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.
Chemical Information
Molecular Weight 511.59
Formula C29H25N3O4S
CAS Number 846557-71-9
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

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, Nrf2, inhibitors, activators

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