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ML385

Cat. No. M8692
ML385 Structure
Size Price Availability Quantity
5mg USD 67.5  USD75 In stock
10mg USD 117  USD130 In stock
25mg USD 252  USD280 In stock
50mg USD 441  USD490 In stock
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Quality Control
Biological Activity

ML385 inihbits the activity of the Nrf2 transcription factor by binding to Neh1, a CNC-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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 511.59
Formula C29H25N3O4S
CAS Number 846557-71-9
Purity 100.00%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C
References

Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors
Anju Singh, et al. ACS Chem Biol. 2016 Nov 18;11(11):3214-3225. PMID: 27552339.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ML385 supplier, Nrf2, inhibitors

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