标签归档：lha

ML334(Synonyms: LH601A)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ML334 (Synonyms: LH601A) 纯度: 99.82%

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。

ML334(Synonyms: LH601A)

ML334 Chemical Structure

CAS No. : 1432500-66-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5450 In-stock
1 mg ￥1850 In-stock
5 mg ￥5550 In-stock
10 mg ￥9500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

ML334 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • NF-κB Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Transcription Factor Targeted Library

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 Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity[1][2].

IC50 & Target

Ki: 1 μM (Keap1)[2]
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[1].
ML334 (LH601A; 50-100 µM; 16 hours; HEK293 cells) treatment induces HO-1 and TRX1 proteins in HEK293 cells[1].
ML334 (LH601A) stimulates NRF2 expression and nuclear translocation in HEK293 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[1]

Cell Line: HEK293 cells
Concentration: 50 μM or 100 µM
Incubation Time: 6 hours, 16 hours
Result: Increased NQO1 and TRX1 mRNAs between 2- and 3-fold at both 6 and 16 h. Enhanced HO-1 mRNA expression between 4- and 7-fold at 6 h.

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 50 μM or 100 µM
Incubation Time: 16 hours
Result: Enhanced HO-1 and TRX1 protein expression at 16 h.

分子量

446.50

Formula

C26H26N2O5
CAS 号

1432500-66-7
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)
溶解性数据
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2396 mL 11.1982 mL 22.3964 mL
5 mM 0.4479 mL 2.2396 mL 4.4793 mL
10 mM 0.2240 mL 1.1198 mL 2.2396 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 (stored under nitrogen)。-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。
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.

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