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ML385 目录号 GC19254

An inhibitor of Nrf2

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5mg
¥515.00
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10mg
¥893.00
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25mg
¥1,943.00
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50mg
¥3,381.00
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100mg
¥6,080.00
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Sample solution is provided at 25 µL, 10mM.

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质量管理

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实验参考方法

Cell experiment:

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[1].

Animal experiment:

Mice: Mice tumor xenografts are randomly allocated into 4 groups: vehicle, ML385, carboplatin, and ML385 in combination with carboplatin. Vehicle, carboplatin (5 mg/kg daily Monday to Friday)18, ML385 (30 mg/kg daily Monday to Friday), or ML385 in combination with carboplatin are administered intraperitoneally for 3 weeks. At the end of treatment period, mice are sacrificed and the tumor, blood, lung, and liver samples are collected[1].

References:

[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]. Xinnong Liu, et al. Isoliquiritigenin ameliorates acute pancreatitis in mice via inhibition of oxidative stress and modulation of the Nrf2/HO-1 pathway. Oxid Med Cell Longev. 20 March 2018.

Chemical Properties

Cas No. 846557-71-9 SDF Download SDF
别名 N/A
化学名 N/A
Canonical SMILES O=C(NC1=NC(C2=CC=C(N(C(C3=C(C)C=CC=C3)=O)CC4)C4=C2)=C(C)S1)CC5=CC(OCO6)=C6C=C5
分子式 C29H25N3O4S 分子量 511.59
溶解度 DMSO : ≥ 30 mg/mL (58.64 mM) 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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产品描述

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

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 uM. A dose-dependent reduction in the NRF2 transcriptional activity is observed and the maximum inhibitory concentration is 5 uM 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].

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].

References:
[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]. Xinnong Liu, et al. Isoliquiritigenin ameliorates acute pancreatitis in mice via inhibition of oxidative stress and modulation of the Nrf2/HO-1 pathway. Oxid Med Cell Longev. 20 March 2018.