1. NF-κB
    Apoptosis
  2. Keap1-Nrf2
    Ferroptosis
  3. ML385

ML385 

目录号: HY-100523 纯度: 99.72%
产品使用指南

ML385是特异的 NRF2 抑制剂,IC50 为1.9 μM。

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ML385 Chemical Structure

ML385 Chemical Structure

CAS No. : 846557-71-9

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥844
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5 mg ¥750
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10 mg ¥1300
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25 mg ¥2850
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50 mg ¥4950
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100 mg ¥8900
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200 mg ¥16000
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500 mg   询价  
1 g   询价  

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 140 篇科研文献

    ML385 purchased from MCE. Usage Cited in: Exp Gerontol. 2017 Dec 15;100:77-86.

    Cells are treated with ML385 at the concentration of 5 μM for 12 h. The expression of Nrf2 and its translocation into nucleus are determined using western blot analysis.

    ML385 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2017 Dec 26;1864(3):882-890.

    RAW264.7 cells are transfected with ML385 (5 μM) in the presence of Tan C (10 μM) for 24 h. Prdx1 and Nrf2 protein expression is determined by Western blotting

    ML385 purchased from MCE. Usage Cited in: Br J Pharmacol. 2018 Oct;175(19):3747-3757.

    Western blot of whole liver homogenate for p-JNK and 3-NT in mice with or without Chloroquine (CQ; 60 mg/kg) at 6 h.

    ML385 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Sep;155:494-509.

    THP-1 cells are incubated with Cardamonin (30 μM), ML385 (5 μM) and ML385 + Cardamonin for 21 h, stimulated with LPS (2 μg/mL) for 3 h, and followed by ATP (5 mM) treatment for 30 min. The protein levels of NLRP3, cleaved caspase-1, ASC and cleaved IL-1β are detected by western blotting assay.

    ML385 purchased from MCE. Usage Cited in: Aging (Albany NY). 2018 Aug 16;10(8):2016-2036.

    Relative changes in the expression of Nrf2, pNrf2 and HO-1 after treatment with D-gal, ML385 alone or combined with lycopene.

    ML385 purchased from MCE. Usage Cited in: Nat Commun. 2018 Oct 24;9(1):4429. 

    QPCR detecting NQO1 and GCLC genes in vector or HPV16 E7-expressing HaCaT cells treated with or without 10 μM ML385 for 24 h.

    ML385 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Dec 13;9:1444.

    Seven days after the last MPTP intoxication, nucleus, and cytosol isolated from SNpc and striatum from all groups (sham, KOK, KOK+ML385, ML385, KOK, ML385) are subjected to Western blot assay to quantify changes in Nrf2 nuclear translocation and NQO1 expression, respectively.

    ML385 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Dec 13;9:1444.

    Seven days after the last MPTP intoxication, SNpc and striatal sections (n = 3 per brain) are subjected to immunofluorescence staining using Nrf2 and NQO1 antibodies with the treatments (sham, KOK, KOK+ML385, ML385, KOK, ML385).

    ML385 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2019 Mar 18;2019:2853534.

    The protein expression levels of Nrf2 (nucleus), Nrf2 (cytoplasm), HO-1, p-NF-κB p65, NF-κB p65, and ICAM-1 proteins are analyzed by Western blot with or without the treatment of H2O2, SAA and ML385.

    ML385 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2019 Apr 7;2019:3501059.

    Western blot of Nrf2 and HO-1 protein expression levels with the treatment of HEMA, HEMA+BHQ, and HEMA+ML385.

    ML385 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2019 Apr 7;2019:3501059.

    Immunofluorescence analysis of Nrf2 expression and nuclear translocation. Green fluorescence represents Nrf2, and blue fluorescence represents nucleus of hDPCs. Data represent mean ± standard deviations (n = 3).
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

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

    IC50 & Target

    IC50: 1.9 μM (NRF2)[1]

    体外研究
    (In Vitro)

    ML385 interacts with NRF2 and affects the DNA binding activity of the NRF2-MAFG protein complex. The addition of ML385 decreases anisotropy in a dose-dependent manner, with an IC50 of 1.9 μM. A dose-dependent reduction in the NRF2 transcriptional activity is observed and the maximum inhibitory concentration is 5 μM by ML385. Treatment with ML385 leads to a significant reduction in NRF2 and downstream target gene expression selectively in KEAP1 mutant H460 cells. ML385 selectively affects the colony forming ability or growth of lung cancer cells with gain of NRF2 function[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    ML385 in combination with carboplatin leads to a significant reduction in tumor cell proliferation, demonstrated by fewer Ki-67 positive cells. Tumor samples treated with ML385 show a significant reduction in NRF2 protein level and its downstream target genes[1].
    ML385 (intraperitoneal injection; 30 mg/kg; 7 days) weakens the therapeutic effects of MSC-Exo on inflammation-induced astrocytic activation in mice, and reduces reactive astrogliosis, NF-κB deactivation[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: 8-week-old C57B/6 male mice[3]
    Dosage: 30 mg/kg; 7 days
    Administration: Intraperitoneal injection
    Result: Reversed inhibition of MSC-Exo on hippocampal astrocytic activation in vivo.
    分子量

    511.59

    Formula

    C29H25N3O4S

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 25 mg/mL (48.87 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9547 mL 9.7735 mL 19.5469 mL
    5 mM 0.3909 mL 1.9547 mL 3.9094 mL
    10 mM 0.1955 mL 0.9773 mL 1.9547 mL
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 15% Solutol HS 15  10% Cremophor EL  35% PEG 400   40% water

      Solubility: 5 mg/mL (9.77 mM); Suspended solution; Need ultrasonic

    • 2.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 3.25 mg/mL (6.35 mM); Suspended solution; Need ultrasonic

      此方案可获得 3.25 mg/mL (6.35 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.89 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.89 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献

    纯度: 99.72%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    ML385
    目录号:
    HY-100523
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