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ML385

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Chemical Structure| 846557-71-9 同义名 : -
CAS号 : 846557-71-9
货号 : A722849
分子式 : C29H25N3O4S
纯度 : 99%+
分子量 : 511.591
MDL号 : MFCD06616124
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(48.87 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 ML385 engages with NRF2, influencing the DNA binding dynamics of the NRF2-MAFG complex. The compound's addition results in a dose-responsive decrease in anisotropy, with an IC50 of 1.9 μM. ML385 induces a dose-dependent diminution of NRF2 transcriptional activity, reaching a peak inhibitory concentration of 5 μM. In KEAP1 mutant H460 cells, ML385 treatment notably lowers the expression of NRF2 and its associated target genes. It also selectively impairs the colony formation and proliferation of lung cancer cells that exhibit increased NRF2 activity. When used alongside carboplatin, ML385 markedly curtails tumor cell growth, as evidenced by a reduced number of Ki-67 positive cells. Tumor specimens treated with ML385 also display a substantial decrease in NRF2 protein levels and the expression of related target genes[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.20mL

9.77mL

1.95mL

0.98mL

19.55mL

3.91mL

1.95mL
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]Xian P, et al. Mesenchymal stem cell-derived exosomes as a nanotherapeutic agent for amelioration of inflammation-induced astrocyte alterations in mice.Theranostics. 2019 Aug 14;9(20):5956-5975.