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ML385

Catalog No. T4360 CAS 846557-71-9

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.

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ML385, CAS 846557-71-9

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 155.00
50 mg	In stock	$ 255.00
100 mg	In stock	$ 396.00
200 mg	In stock	$ 592.00
500 mg	In stock	$ 947.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 100%

Purity: 99.85%

Purity: 99.76%

Purity: 99.49%

Purity: 98.88%

Purity: 98.86%

Biological Description

Chemical Properties

Storage & Solubility Information

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: 30 mg/mL

References and Literature

1. Singh A, et al. Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors. ACS Chem Biol. 2016 Nov 18;11(11):3214-3225. 2. Ji L, et al. The NRF2 antagonist ML385 inhibits PI3K-mTOR signaling and growth of lung squamous cell carcinoma cells. Cancer Med. 2023 Mar;12(5):5688-5702. 3. Szewczyk-Golec K, et al. Strategies for Modulating Oxidative Stress under Diverse Physiological and Pathological Conditions. Oxid Med Cell Longev. 2018 Dec 30;2018:3987941. 4. Wu Y, Zeng S, Wan B, et al. Sophoricoside attenuates lipopolysaccharide-induced acute lung injury by activating the AMPK/Nrf2 signaling axis[J]. International Immunopharmacology. 2021, 90: 107187 5. Wu Y, Zeng S, Wan B, et al. Sophoricoside attenuates lipopolysaccharide-induced acute lung injury by activating the AMPK/Nrf2 signaling axis[J]. International Immunopharmacology. 2020: 107187. 6. Chen X, Liang H, Xi Z, et al. BM-MSC Transplantation Alleviates Intracerebral Hemorrhage-Induced Brain Injury, Promotes Astrocytes Vimentin Expression, and Enhances Astrocytes Antioxidation via the Cx43/Nrf2/HO-1 Axis[J]. Frontiers in Cell and Developmental Biology. 2020, 8: 302.

Citations

1. Jiang H, Lin C, Cai T, et al.Taxifolin‐mediated Nrf2 activation ameliorates oxidative stress and apoptosis for the treatment of glucocorticoid‐induced osteonecrosis of the femoral head.Phytotherapy Research.2023 2. Tao M, Yan W, Chen C, et al.Omentin-1 ameliorates experimental inflammatory bowel disease via Nrf2 activation and redox regulation.Life Sciences.2023: 121847. 3. Jin B, Chen Y, Wang J, et al.Costunolide alleviates hyperglycaemia‐induced diabetic cardiomyopathy via inhibiting inflammatory responses and oxidative stress.Journal of Cellular and Molecular Medicine.2023 4. Zhang L, Hu C, Jin B, et al.Bicyclol Alleviates Streptozotocin-induced Diabetic Cardiomyopathy By Inhibiting Chronic Inflammation And Oxidative Stress.Cardiovascular Drugs and Therapy.2023: 1-14. 5. Lan J, Zhou Y, Wang H, et al.Protective Effect of Human Umbilical Cord Mesenchymal Stem Cell Derived Conditioned Medium in a Mutant TDP-43 Induced Motoneuron-Like Cellular Model of ALS.Brain Research Bulletin.2022 6. Fan P, Lu Y, Wei H, et al.Metformin attenuates sevoflurane-induced neurogenesis damage and cognitive impairment: involvement of the Nrf2/G6PD pathway.Metabolic Brain Disease.2023: 1-17. 7. Zheng W, Yang H, Lin H, et al.ML385 suppresses the proliferation, migration, and invasion of thyroid carcinoma cells by impairing aerobic glycolysis.Molecular & Cellular Toxicology.2023: 1-10. 8. Chen F, Zhu J, Wang W. Ulinastatin Attenuates LPS-Induced Inflammation and Inhibits Endoplasmic Reticulum Stress–Induced Apoptosis in Renal Tubular Epithelial Cells via Regulation of the TLR4/NF-κB and Nrf2/HO-1 Pathways. Inflammation. 2021: 1-10. 9. Liu Y, Hou M, Pan Z, et al. Arctiin-reinforced antioxidant microcarrier antagonizes osteoarthritis progression. Journal of Nanobiotechnology. 2022, 20(1): 1-20 10. Wu Y, Zeng S, Wan B, et al. Sophoricoside attenuates lipopolysaccharide-induced acute lung injury by activating the AMPK/Nrf2 signaling axis. International Immunopharmacology. 2021, 90: 107187

11. Chen Y, Shi J, Wang X, et al.An antioxidant feedforward cycle coordinated by linker histone variant H1. 2 and NRF2 that drives nonsmall cell lung cancer progression.Proceedings of the National Academy of Sciences.2023, 120(39): e2306288120. 12. Chen X, Liang H, Xi Z, et al. BM-MSC Transplantation Alleviates Intracerebral Hemorrhage-Induced Brain Injury, Promotes Astrocytes Vimentin Expression, and Enhances Astrocytes Antioxidation via the Cx43/Nrf2/HO-1 Axis. Frontiers in Cell and Developmental Biology. 2020, 8: 302 13. Chen Z, Wang H, Hu B, et al. Transcription factor nuclear factor erythroid 2 p45-related factor 2 (NRF2) ameliorates sepsis-associated acute kidney injury by maintaining mitochondrial homeostasis and improving the mitochondrial function. European Journal of Histochemistry. 2022, 66(3) 14. Zhang H, Chen C, Liu Y, et al. NRF-2/HO-1 Pathway-Mediated SHOX2 Activation Is a Key Switch for Heart Rate Acceleration by Yixin-Fumai Granules. Oxidative Medicine and Cellular Longevity. 2022 15. Cao L, Zhao J, Ma L, et al. Lycopene attenuates zearalenone-induced oxidative damage of piglet sertoli cells through the nuclear factor erythroid-2 related factor signaling pathway. Ecotoxicology and Environmental Safety. 2021, 225: 112737. 16. Wang N, Nie H, Zhang Y, et al. Dexmedetomidine exerts cerebral protective effects against cerebral ischemic injury by promoting the polarization of M2 microglia via the Nrf2/HO-1/NLRP3 pathway. Inflammation Research. 2021: 1-14. 17. Zhang Q, Bai X, Wang R, et al. 4‐octyl Itaconate inhibits lipopolysaccharide (LPS)‐induced osteoarthritis via activating Nrf2 signalling pathway. Journal of Cellular and Molecular Medicine. 2022 18. Wu Y, Wang Y, Gao Z, et al. Ethyl ferulate protects against lipopolysaccharide-induced acute lung injury by activating AMPK/Nrf2 signaling pathway. Acta Pharmacologica Sinica. 2021, 42(12): 2069-2081. 19. Wen H, Zhang X, Li Q, et al. Ruscogenins Improve CD-Like Enteritis by Inhibiting Apoptosis of Intestinal Epithelial Cells and Activating Nrf2/NQO1 Pathway. Oxidative Medicine and Cellular Longevity. 2022 20. Lin Y, Luo T, Weng A, et al. Gallic Acid Alleviates Gouty Arthritis by Inhibiting NLRP3 Inflammasome Activation and Pyroptosis Through Enhancing Nrf2 Signaling. Frontiers in Immunology. 2020 Dec 7;11:580593. doi: 10.3389 21. Xue J, Liao Q, Luo M, et al. Cigarette smoke-induced oxidative stress activates NRF2 to mediate fibronectin disorganization in vascular formation. Open Biology. 2022, 12(4): 210310 22. Shi B, Hao Y, Li W, et al. TIPE2 May Target the Nrf2/HO-1 Pathway to Inhibit M1 Macrophage–Related Neutrophilic Inflammation in Asthma. Frontiers in Immunology. 2022, 13 23. Li X, Qin X, Tian J, et al. Liquiritin protects PC12 cells from corticosterone-induced neurotoxicity via regulation of metabolic disorders, attenuation ERK1/2-NF-κB pathway, activation Nrf2-Keap1 pathway, and inhibition mitochondrial apoptosis pathway. Food and Chemical Toxicology. 2020: 111801 24. Chen W, Ye Y, Wu Z, et al. Temporary Upregulation of Nrf2 by Naringenin Alleviates Oxidative Damage in the Retina and ARPE-19 Cells. Oxidative Medicine and Cellular Longevity. 2021, 2021. 25. Li D, Xu Z, Li Y, et al.Breviscapine attenuates lead‑induced myocardial injury by activating the Nrf2 signaling pathway.Experimental and Therapeutic Medicine.2024, 27(1): 1-8. 26. Wang J, Jin B, Chen Y, et al.Costunolide attenuates high‐fat diet‐induced inflammation and oxidative stress in non‐alcoholic fatty liver disease.Drug Development Research.2024, 85(1): e22150. 27. Zhu M, Zhao T, Zha B, et al.Piceatannol protects against myocardial ischemia/reperfusion injury by inhibiting ferroptosis via Nrf-2 signaling-mediated iron metabolism.Biochemical and Biophysical Research Communications.2024: 149598. 28. Yin Z, Zhang J, Zhao M, et al.Maresin‐1 ameliorates hypertensive vascular remodeling through its receptor LGR6.MedComm.2024, 5(3): e491. 29. Chen X, Zhou Q, Chen H, et al.Glutathione Induces Keap1 S-Glutathionylation and Mitigates Oscillating Glucose-Induced β-Cell Dysfunction by Activating Nrf2.Antioxidants.2024, 13(4): 400.

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Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library Cell Cycle Compound Library Bioactive Compounds Library Max Transcription Factor-Targeted Compound Library Anti-Alzheimer's Disease Compound Library Anti-Obesity Compound Library Oxidation-Reduction Compound Library Antioxidant Compound Library PPI Inhibitor Library

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Keywords

ML385 846557-71-9 Apoptosis Immunology/Inflammation Others Ferroptosis Nrf2 Inhibitor inhibit ML 385 ML-385 Keap1-Nrf2 inhibitor

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