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ML385

产品编号 T4360 CAS 846557-71-9

ML385 是一种 NRF2 抑制剂 (IC50=1.9 μM)，具有新颖性和特异性。ML385 通过抑制 NRF2 调控抗氧化应激，具有抗炎活性。ML385 还具有抗肿瘤活性。

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

ML385, CAS 846557-71-9

规格	价格/CNY	货期
1 mg	￥ 247	现货
5 mg	￥ 619	现货
10 mg	￥ 1,070	现货
25 mg	￥ 1,950	现货
50 mg	￥ 2,730	现货
100 mg	￥ 3,990	现货
200 mg	￥ 5,790	现货
500 mg	￥ 8,860	现货
1 mL * 10 mM (in DMSO)	￥ 686	现货

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选择批次

纯度: 100%

COA DATASHEET SDS HPLC HNMR

纯度: 99.85%

COA DATASHEET SDS HPLC HNMR

纯度: 99.76%

COA DATASHEET SDS LCMS HNMR

纯度: 99.49%

COA DATASHEET SDS HPLC HNMR

纯度: 98.88%

COA DATASHEET SDS HPLC HNMR

纯度: 98.86%

COA DATASHEET SDS HPLC HNMR

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 30 mg/mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

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.

文献引用

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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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

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

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

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产品描述	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.
靶点活性	Nrf2:1.9 μM
体外活性	方法：人肺癌细胞 A549 用 ML385 (0.25-5 μM) 处理 12-72 h，使用 RT-qPCR 方法检测靶基因表达水平。结果：ML385 剂量依赖性和时间依赖性降低 NRF2 的转录活性。[1] 方法：人肺癌细胞 EBC1 用 ML385 (1-25 μM) 处理 48 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：用 5 μM ML385 处理抑制 NRF2 表达。当 ML385 浓度上升到 5 μM 以上时，NRF2 蛋白水平开始恢复。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 ML385 (30 mg/kg) 和 carboplatin (5 mg/kg) 腹腔注射给携带人肺癌肿瘤 A549 或 H460 的 athymic nude 小鼠，每周五次，持续三周。结果：用 ML385 与 carboplatin 联合治疗显示出肿瘤生长的显著减少。尽管用单一药物治疗导致肿瘤生长减少，但这些影响的大小在细胞系之间是可变的，并且没有达到统计学意义。[1] 方法：为研究 Nrf2 是否通过铁死亡调节急性肝功能衰竭 (ACLF)，将 ML385 (30 mg/kg) 腹腔注射给构建 ACLF 模型的 BALB/c 小鼠，每周四次，持续四周。结果：与 ACLF组相比，ML385 组观察到更严重的组织病理学病变。Nrf2 抑制剂 ML385 加重了脂质过氧化和肝损伤。[3]
细胞实验	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
动物实验	Mice tumor xenografts are administered intraperitoneally ML385 (30 mg/kg).

分子量	511.59
分子式	C29H25N3O4S
CAS No.	846557-71-9

ML385

存储

溶解度

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

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剂量换算

体内实验配液计算器

技术支持

Keywords