NRF2 Inhibitor(ML385),IC-0199622

ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 ¦ÌM

Product Introduction
ML385 is a potent and selective small-molecule inhibitor of nuclear factor erythroid 2-related factor 2 (NRF2). NRF2 is a key transcription factor that regulates the expression of antioxidant response element (ARE)-dependent genes, protecting cells from oxidative stress and xenobiotic damage. In many cancers, constitutive NRF2 activation promotes tumor cell survival, chemoresistance, and metabolic reprogramming. ML385 binds to the NRF2 protein and inhibits its transcriptional activity by interfering with NRF2-DNA binding and NRF2-MAFG complex formation. It has demonstrated anti-tumor activity in NRF2-dependent cancer models, including non-small cell lung cancer, by sensitizing cells to chemotherapeutic agents and suppressing tumor growth. ML385 is a valuable pharmacological tool for studying NRF2 signaling, oxidative stress responses, and NRF2-targeted therapeutic strategies.

Product Features
1. Potent NRF2 Inhibitor: Selectively inhibits NRF2 transcriptional activity with an IC₅₀ in the submicromolar range.
2. Selective Mechanism: Interferes with NRF2-DNA binding and NRF2-MAFG complex formation.
3. Anti-Tumor Activity: Suppresses proliferation and sensitizes NRF2-dependent cancer cells to chemotherapy.
4. Research Tool: Widely used for studying NRF2 signaling in cancer and oxidative stress research.
5. High Purity: Supplied at high purity suitable for reproducible pharmacological studies.

Specifications
Size: 100 mg / 500 mg
Purity: ¡Ý98%
Solubility: DMSO: ¡Ý20 mg/mL
Molecular Weight: 507.57
Molecular Formula: C28H25N5O3S

Storage and Stability
Storage Conditions: Store at -20¡ãC, protected from light and moisture.
Shelf Life: The product is stable for 24 months from the date of manufacture when stored as directed. For reconstituted solutions, aliquot and store at -20¡ãC. Avoid repeated freeze-thaw cycles.

Protocol (For Reference Only)
Important: Protect from light and moisture during handling and storage. Prepare stock solutions in anhydrous DMSO.
1. Stock Solution Preparation: Dissolve ML385 in anhydrous DMSO to prepare a concentrated stock solution (e.g., 10-50 mM). Aliquot into single-use vials and store at -20¡ãC protected from light.
2. In Vitro Working Solution Preparation: Dilute DMSO stock solution into culture medium to achieve working concentrations typically ranging from 1-20 µM. Limit final DMSO concentration to ¡Ü0.1%.
3. NRF2 Inhibition Assay: Treat cells with ML385 at 1-10 µM for 24-48 hours. Assess NRF2 transcriptional activity by measuring expression of NRF2 target genes (e.g., NQO1, HO-1, GCLM) by qPCR or Western blot.
4. Chemosensitization Studies: Combine ML385 with chemotherapeutic agents (e.g., cisplatin, carboplatin) in NRF2-dependent cancer cells. Assess synergistic effects by cell viability or apoptosis assays.
5. Oxidative Stress Studies: Treat cells with ML385 and measure intracellular reactive oxygen species levels using fluorescent probes.

Precautions
1. Protect from light and moisture during handling and storage.
2. Use appropriate vehicle controls; DMSO concentration should not exceed 0.1%.
3. ML385 exhibits differential potency across cell types depending on NRF2 expression and dependence.
4. For research use only. Not for use in diagnostic or therapeutic procedures.

FAQ (Simplified)
Q1: What is the recommended concentration for NRF2 inhibition in vitro?
A1: ML385 at 1-10 µM effectively inhibits NRF2 activity in most cell types. For complete inhibition, 5-10 µM is commonly used.
Q2: How does ML385 inhibit NRF2?
A2: ML385 binds to NRF2 and inhibits its transcriptional activity by interfering with NRF2-DNA binding and NRF2-MAFG complex formation.
Q3: How should I store ML385?
A3: Store at -20¡ãC protected from light and moisture. Aliquot reconstituted solutions and avoid repeated freeze-thaw cycles.

Disclaimer
1. For Research Use Only. Not for use in diagnostic or therapeutic procedures.
2. Due to the variable nature of biological research, optimization of conditions is recommended.
3. This warranty is limited to the replacement of the product. The manufacturer assumes no liability for incidental or consequential damages.
4. Wear appropriate protective clothing and gloves when handling this product.

Ordering Information
Catalog Number: IC-0199622
Product Name: NRF2 Inhibitor (ML385)
Size: 100 mg / 500 mg
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