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CAS No.: 846557-71-9

ML385 Catalog No. CSN22320

Synonyms: ML385

ML-385 is a selective inhibitor of NRF2 via binding to Neh1 DNA binding domain with IC50 of 1.9 µM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述ML385 is a novel and specific NRF2 inhibitor which can inhibit the activity of the Nrf2 transcription factor by binding to Neh1. ML385 led a dose-dependent reduction in the NRF2 transcriptional activity with maximum inhibitory concentration at 5μM in A549 cells post 72-hour exposure. And the reduction of Nrf2 on protein level could be observed in A549 cells post 24 or 48-hour treatment with 5μM and 10μM ML385. Combination of ML385 at concentration of 1 or 5μM with Carboplatin, doxorubicin or taxol significantly enhanced cytotoxicity in A549 and H460 cell, compared with treatment with the agent alone. Consistent with this in vitro study, intraperitoneal administration of 30mg/kg ML385, once daily, 5 days per week, for 3 weeks, in combination with carboplatin significantly reduced the tumor growth in subcutaneous H460 lung tumor xenografts. Also a significant anti-tumor efficacy of ML385 in combination with carboplatin in an orthotopic A549 lung tumor model could be observed. ML385 may not be across blood brain barrier.
动物研究
剂量
Mice: 30 mg/kg^[1] (i.p.), 40 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 30 mg/kg^[1] (i.p.), 40 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Singh A, Venkannagari S, Oh KH, Zhang YQ, Rohde JM, Liu L, Nimmagadda S, Sudini K, Brimacombe KR, Gajghate S, Ma J, Wang A, Xu X, Shahane SA, Xia M, Woo J, Mensah GA, Wang Z, Ferrer M, Gabrielson E, Li Z, Rastinejad F, Shen M, Boxer MB, Biswal S. Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors. ACS Chem Biol. 2016 Nov 18;11(11):3214-3225. doi: 10.1021/acschembio.6b00651. Epub 2016 Oct 17. PMID: 27552339; PMCID: PMC5367156.
[2] Yan M, Ye L, Yin S, Lu X, Liu X, Lu S, Cui J, Fan L, Kaplowitz N, Hu H. Glycycoumarin protects mice against acetaminophen-induced liver injury predominantly via activating sustained autophagy. Br J Pharmacol. 2018 Oct;175(19):3747-3757. doi: 10.1111/bph.14444. Epub 2018 Aug 21. PMID: 30024038; PMCID: PMC6135785.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9547 mL
- 9.7734 mL
- 19.5468 mL
- 5 mM
- 0.3909 mL
- 1.9547 mL
- 3.9094 mL
- 10 mM
- 0.1955 mL
- 0.9773 mL
- 1.9547 mL

技术信息

CAS号

846557-71-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H25N3O4S

运输

蓝冰

分子量

511.59

别名

ML385

溶解度

DMSO	50.0 mg/mL (97.7 mM)

动物实验配方

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ML385 Catalog No. CSN22320

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