ML334 (Synonyms: LH601A)
目录号: PL01842 纯度: ≥99%
CAS No. :1432500-66-7
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中文名称
ML334
英文名称
ML334
英文别名
LH601A;ML334;(1S,2R)-2-[[(1S)-1-[(1,3-dioxo-2-isoindolyl)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-oxomethyl]-1-cyclohexanecarboxylic acid;(1s,2r)-2-{[(1s)-1-[(1,3-Dioxo-1,3-Dihydro-2h-Isoindol-2-Yl)methyl]-3,4-Dihydroisoquinolin-2(1h)-Yl]carbonyl}cyclohexanecarboxylic Acid;4l7b;MLS004683641;BDBM50109398;SMR003455734
Cas No.
1432500-66-7
分子式
C26H26N2O5
分子量
446.50
包装储存
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
产品详情
ML334 (LH601A) 是一种有效的,细胞可渗透的 NRF2 激活剂,通过抑制 Keap1-NRF2 蛋白质相互作用来发挥作用。ML334 以 Kd 值为 1μM 来结合 Keap1 Kelch 域。ML334 刺激 NRF2 表达和核易位并诱导抗氧化反应元件 (ARE) 活性。
生物活性
ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a K d of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
性状
Solid
IC50 & Target[1][2]
Ki: 1 μM (Keap1)
体外研究(In Vitro)
ML334 (LH601A; 50-100 μM; 6-16 hours; HEK293 cells) treatment increases NQO1 and TRX1 mRNAs between 2- and 3-fold at both 6 and 16 h. And also enhances HO-1 mRNA expression between 4- and 7-fold at 6 h, with lesser fold-changes at 16 h.
ML334 (LH601A; 50-100 μM; 16 hours; HEK293 cells) treatment induces HO-1 and TRX1 proteins in HEK293 cells.
ML334 (LH601A) stimulates NRF2 expression and nuclear translocation in HEK293 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Wen X, et al. Activation of NRF2 Signaling in HEK293 Cells by a First-in-Class Direct KEAP1-NRF2 Inhibitor. J Biochem Mol Toxicol. 2015 Jun;29(6):261-6.
[2]. Hu L, et al. Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. Bioorg Med Chem Lett. 2013 May 15;23(10):3039-43.
溶解度数据
In Vitro: DMSO : 44.65 mg/mL (100.00 mM; Need ultrasonic)Ethanol : 44.65 mg/mL (100.00 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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